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The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase.
Antimicrob Agents Chemother 52: 458-64 (2008)
Pharmasset
Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human pancreatic cancer toxicity.
J Med Chem 50: 6316-25 (2007)
University Of Manchester
Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds.
Bioorg Med Chem Lett 18: 423-6 (2008)
University Of Bologna
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
Bioorg Med Chem Lett 18: 256-61 (2008)
F. Hoffmann-La Roche
Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.
Bioorg Med Chem 16: 909-21 (2008)
Kissei Pharmaceutical
2D QSAR and similarity studies on cruzain inhibitors aimed at improving selectivity over cathepsin L.
Bioorg Med Chem 16: 838-53 (2008)
Universidade De S£O Paulo
Cytochrome P3A4 inhibitors and other constituents of Fibraurea tinctoria.
J Nat Prod 70: 1930-3 (2007)
National Cheng Kung University
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors.
J Med Chem 50: 6367-82 (2007)
Nitromed
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
J Med Chem 50: 6356-66 (2007)
Neurocrine Biosciences
Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine.
J Med Chem 50: 6383-91 (2007)
Research Triangle Institute
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
J Med Chem 50: 6303-6 (2007)
Merck Research Laboratories
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines.
Bioorg Med Chem 16: 1242-53 (2008)
Universite Paris 7-Denis Diderot
Discovery of potent& selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis.
J Med Chem 50: 6095-103 (2007)
Pfizer
Characterization of thyroid hormone receptor alpha (TRalpha)-specific analogs with varying inner- and outer-ring substituents.
Bioorg Med Chem 16: 762-70 (2008)
University Of California San Francisco
Discovery of new MurF inhibitors via pharmacophore modeling and QSAR analysis followed by in-silico screening.
Bioorg Med Chem 16: 1218-35 (2008)
University Of Jordan
Synthesis and evaluation of novel aromatic substrates and competitive inhibitors of GABA aminotransferase.
Bioorg Med Chem Lett 18: 3122-5 (2008)
Northwestern University
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
Bioorg Med Chem Lett 18: 215-9 (2008)
Schering-Plough Research Institute
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.
Eur J Med Chem 43: 1304-8 (2008)
University Of Maryland
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
J Med Chem 50: 5886-9 (2007)
Pfizer
Solution-phase parallel synthesis of carbamates as gamma-secretase inhibitors.
J Comb Chem 10: 56-62 (2008)
Schering-Plough Research Institute
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.
J Nat Prod 70: 1691-5 (2007)
Seoul National University
New potent indole derivatives as hyaluronidase inhibitors.
Chem Biol Drug Des 70: 547-51 (2007)
TBA
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
J Med Chem 50: 5912-25 (2007)
Astrazeneca Pharmaceuticals
Discovery of a novel warhead against beta-secretase through fragment-based lead generation.
J Med Chem 50: 5903-11 (2007)
Astrazeneca R&D
Design and synthesis of indole-based peptoids as potent noncompetitive antagonists of transient receptor potential vanilloid 1.
J Med Chem 50: 6133-43 (2007)
University Of Barcelona
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.
J Med Chem 50: 5976-83 (2007)
Georgetown University Medical Center
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Bioorg Med Chem 16: 1359-75 (2008)
Osi Pharmaceuticals
Synthesis and characterization of carnitine nitro-derivatives.
Bioorg Med Chem 16: 1444-51 (2008)
University Of Perugia
Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter.
Bioorg Med Chem 16: 783-93 (2008)
Emory University
Substituted 2-oxo-azepane derivatives are potent, orally active gamma-secretase inhibitors.
Bioorg Med Chem Lett 18: 304-8 (2008)
F. Hoffmann-La Roche
Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening.
Bioorg Med Chem Lett 18: 285-8 (2008)
Gakushuin University
Surveying polypeptide and protein domain conformation and association with FlAsH and ReAsH.
Nat Chem Biol 3: 779-84 (2007)
Yale University
Model structure of the Na+/H+ exchanger 1 (NHE1): functional and clinical implications.
J Biol Chem 282: 37854-63 (2007)
Tel-Aviv University
Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors.
Bioorg Med Chem Lett 18: 402-4 (2008)
The University Of Sydney
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.
Bioorg Med Chem Lett 18: 324-8 (2008)
Gsk
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.
Eur J Med Chem 43: 1469-77 (2008)
Université
GRIND-based 3D-QSAR to predict inhibitory activity for similar enzymes, OSC and SHC.
Eur J Med Chem 43: 1462-8 (2008)
Casmedchem Laboratory
Synthesis and biological activity of imidazopyridine anticoccidial agents: Part II.
Eur J Med Chem 43: 1123-51 (2008)
Scynexis
Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.
Eur J Med Chem 43: 1478-88 (2008)
Freie UniversitäT Berlin
Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure.
Bioorg Med Chem 16: 1299-308 (2008)
Dainippon Sumitomo Pharma
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Bioorg Med Chem 16: 1279-86 (2008)
Mclean Hospital
Design, synthesis, FGF-1 binding, and molecular modeling studies of conformationally flexible heparin mimetic disaccharides.
Bioorg Med Chem Lett 18: 344-9 (2008)
Progen Pharmaceuticals
1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke.
Bioorg Med Chem Lett 18: 409-13 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Combined 3D QSAR and molecular docking studies to reveal novel cannabinoid ligands with optimum binding activity.
Bioorg Med Chem Lett 17: 6754-63 (2007)
The National Hellenic Research Foundation
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Bioorg Med Chem Lett 17: 6841-6 (2007)
Eli Lilly
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.
Bioorg Med Chem Lett 18: 418-22 (2008)
Schering-Plough Research Institute
Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs).
Bioorg Med Chem Lett 18: 405-8 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model.
J Med Chem 50: 5951-66 (2007)
Zydus Research Centre
Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone.
Bioorg Med Chem 16: 1309-18 (2008)
Korea Food Research Institute
Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.
Bioorg Med Chem 16: 1376-92 (2008)
University Of Minnesota
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.
Bioorg Med Chem 16: 650-7 (2008)
Kyoto University
N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors.
Bioorg Med Chem Lett 17: 6729-33 (2007)
Methylgene
Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain.
Bioorg Med Chem Lett 17: 6697-700 (2007)
Universitat Jaume I
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors.
Bioorg Med Chem Lett 17: 6707-13 (2007)
Pfizer
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.
Bioorg Med Chem Lett 17: 6691-6 (2007)
Pfizer
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
Eur J Med Chem 43: 1152-9 (2008)
Johannes Gutenberg University
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
J Med Chem 50: 5967-75 (2007)
University Of Southern California
Multiple N-methylation by a designed approach enhances receptor selectivity.
J Med Chem 50: 5878-81 (2007)
Technische UniversitäT MüNchen
Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).
J Med Chem 50: 5890-3 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
J Med Chem 50: 6265-73 (2007)
Abbott Laboratories
Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
J Med Chem 50: 6059-66 (2007)
Cancercare Manitoba
Interactions of methylene blue with human disulfide reductases and their orthologues from Plasmodium falciparum.
Antimicrob Agents Chemother 52: 183-91 (2007)
Biochemie-Zentrum Der Universit£T Heidelberg
Madurahydroxylactone derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and RNase H.
Antimicrob Agents Chemother 52: 361-4 (2008)
National Cancer Institute
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
Antimicrob Agents Chemother 52: 225-36 (2008)
Imquest Biosciences
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
Antimicrob Agents Chemother 52: 157-63 (2008)
University Of Pittsburgh School Of Medicine
Synthesis and heparanase inhibitory activity of sulfated mannooligosaccharides related to the antiangiogenic agent PI-88.
Bioorg Med Chem 16: 699-709 (2008)
Progen Pharmaceuticals
Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents.
Bioorg Med Chem 16: 771-82 (2008)
Universidade Federal Do Rio Grande Do Sul (Ufrgs)
Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.
Bioorg Med Chem Lett 17: 6887-90 (2007)
Pfizer
Structure-activity relationships of adenosines with heterocyclic N6-substituents.
Bioorg Med Chem Lett 17: 6779-84 (2007)
Monash University (Parkville Campus)
5'-O-[(N-acyl)sulfamoyl]adenosines as antitubercular agents that inhibit MbtA: an adenylation enzyme required for siderophore biosynthesis of the mycobactins.
J Med Chem 50: 6080-94 (2007)
University Of Minnesota
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
J Med Chem 50: 6144-53 (2007)
University M£Nster
Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.
Bioorg Med Chem 16: 739-45 (2008)
University Of South Carolina
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.
Bioorg Med Chem 16: 981-94 (2008)
Nippon Shinyaku
Spermatinamine, the first natural product inhibitor of isoprenylcysteine carboxyl methyltransferase, a new cancer target.
Bioorg Med Chem Lett 17: 6860-3 (2007)
Griffith University
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1.
Bioorg Med Chem Lett 17: 6811-5 (2007)
F. Hoffmann-La Roche
Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.
Bioorg Med Chem Lett 17: 6832-5 (2007)
Cardiff University
Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).
Bioorg Med Chem 16: 209-21 (2008)
Lek Pharmaceuticals
Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.
Bioorg Med Chem 16: 902-8 (2008)
Sapienza University Of Rome
Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs.
Bioorg Med Chem 16: 746-54 (2008)
Research Triangle Institute
Discovery of small-molecule inhibitors of tyrosinase.
Bioorg Med Chem Lett 17: 6871-5 (2007)
University Of Texas Southwestern Medical Center
Development of CXCR3 antagonists. Part 2: Identification of 2-amino(4-piperidinyl)azoles as potent CXCR3 antagonists.
Bioorg Med Chem Lett 17: 6806-10 (2007)
Ucb Pharma
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.
Bioorg Med Chem Lett 17: 6825-31 (2007)
Neurocrine Biosciences
Structure activity relationships of quinoline-containing c-Met inhibitors.
Eur J Med Chem 43: 1321-9 (2008)
Pfizer
Activity of sulfonium bisphosphonates on tumor cell lines.
J Med Chem 50: 6067-79 (2007)
University Of Illinois At Urbana-Champaign
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
J Med Chem 50: 5882-5 (2007)
Astrazeneca R&D Charnwood
Discovery of 5-Substituted-6-chlorouracils as Efficient Inhibitors of Human Thymidine Phosphorylase.
J Med Chem 50: 6016-23 (2007)
Gilead Sciences
Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors.
J Biol Chem 282: 36905-13 (2007)
University Of Utah
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
Bioorg Med Chem 16: 869-73 (2008)
University Of Maryland
Discovery of long-acting N-(cyanomethyl)-N-alkyl-L-prolinamide inhibitors of dipeptidyl peptidase IV.
Bioorg Med Chem 16: 190-208 (2008)
Minase Research Institute
Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta.
Chem Biol 14: 1186-97 (2007)
University Of Virginia At Charlottesville
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
J Med Chem 50: 6154-64 (2007)
University Of Wisconsin-Madison
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.
J Med Chem 50: 6004-15 (2007)
Universidad De La RepúBlica
Cytotoxic metabolites from an Indonesian sponge Lendenfeldia sp.
J Nat Prod 70: 1824-6 (2007)
University Of Mississippi
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.
J Med Chem 50: 5568-70 (2007)
University Of Antwerp
Discovery of small molecule CXCR4 antagonists.
J Med Chem 50: 5655-64 (2007)
Emory University
Probing Binding Requirements of Type I and Type II Isoforms of Inosine Monophosphate Dehydrogenase with Adenine-Modified Nicotinamide Adenine Dinucleotide Analogues.
J Med Chem 50: 5743-5751 (2007)
University Of Minnesota At Twin Citiies
The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.
J Med Chem 50: 5720-5726 (2007)
University Of Southampton
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.
Proc Natl Acad Sci U S A 104: 17335-40 (2007)
Istituto Di Ricerche Di Biologia Molecolare
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET.
J Med Chem 50: 5752-64 (2007)
University Hospital Of The Westf£Lische Wilhelms-Universit£T M£Nster
Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.
J Med Chem 50: 5644-54 (2007)
Università
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.
J Med Chem 50: 5853-7 (2007)
Memorial Sloan-Kettering Cancer Center
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
Proc Natl Acad Sci U S A 104: 17347-52 (2007)
Institut National De La Sant£
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
Antimicrob Agents Chemother 52: 128-36 (2008)
Duke University Medical Center
In silico screening of HIV-1 non-nucleoside reverse transcriptase and protease inhibitors.
Eur J Med Chem 43: 1412-22 (2008)
Universidade Federal De Minas Gerais
Acetyl-lysine analog peptides as mechanistic probes of protein deacetylases.
J Biol Chem 282: 37256-65 (2007)
University Of Wisconsin-Madison
Synthesis and structure-activity relationships of N-{1-[(6-fluoro-2-naphthyl)methyl]piperidin-4-yl}benzamide derivatives as novel CCR3 antagonists.
Bioorg Med Chem 16: 144-56 (2008)
Astellas Pharma
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.
Bioorg Med Chem Lett 17: 6463-6 (2007)
The Scripps Research Institute
Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 17: 6472-5 (2007)
University Of Southern California
Structure of a novel thrombin inhibitor with an uncharged D-amino acid as P1 residue.
Eur J Med Chem 43: 1330-5 (2008)
Institut FüR Biochemie
Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues.
Bioorg Med Chem Lett 17: 6434-8 (2007)
Université
Synthesis, anti-HIV-1 integrase, and cytotoxic activities of 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives.
Eur J Med Chem 43: 1188-98 (2008)
Medical University Of Gdansk
Vanillic acid derivatives from the green algae Cladophora socialis as potent protein tyrosine phosphatase 1B inhibitors.
J Nat Prod 70: 1790-2 (2007)
Griffith University
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.
Biochemistry 46: 13019-30 (2007)
Pfizer
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis.
J Med Chem 50: 5735-42 (2007)
University Of Kansas
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin.
J Med Chem 50: 5863-5867 (2007)
University Of California Davis
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
J Med Chem 50: 5535-8 (2007)
Wyeth Research
Design of mechanism-based inhibitors of transthyretin amyloidosis: studies with biphenyl ethers and new structural templates.
J Med Chem 50: 5589-99 (2007)
Institute Of Sciences
Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase.
J Med Chem 50: 5712-9 (2007)
Pfizer
Mechanisms, biology and inhibitors of deubiquitinating enzymes.
Nat Chem Biol 3: 697-705 (2007)
Institute For Bio-Medical Research
First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.
J Med Chem 50: 5685-95 (2007)
University Of Bonn
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.
Bioorg Med Chem Lett 17: 6584-7 (2007)
Glaxosmithkline
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.
Bioorg Med Chem Lett 17: 6623-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
Bioorg Med Chem Lett 17: 6505-10 (2007)
Universit£
Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues.
Bioorg Med Chem Lett 17: 6439-43 (2007)
Universidad De Navarra
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
J Med Chem 50: 5543-6 (2007)
Methylgene
Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors.
J Med Chem 50: 5547-9 (2007)
Wyeth Research
Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.
J Med Chem 50: 5727-34 (2007)
St. Jude Research Hospital
New iantherans from the marine sponge Ianthella quadrangulata: novel agonists of the P2Y(11) receptor.
J Med Chem 50: 5600-7 (2007)
University Of Bonn
Phenotypic characterization of resistant Val36 variants of hepatitis C virus NS3-4A serine protease.
Antimicrob Agents Chemother 52: 110-20 (2008)
Vertex Pharmaceuticals
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
Bioorg Med Chem 16: 276-83 (2008)
The University Of The West Indies
Design, synthesis, and preliminary evaluation of 4-(6-(3-nitroguanidino)hexanamido)pyrrolidine derivatives as potential iNOS inhibitors.
Bioorg Med Chem 16: 578-85 (2008)
Shandong University
Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.
Bioorg Med Chem Lett 17: 6448-54 (2007)
Astrazeneca
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 17: 6476-80 (2007)
Bristol-Myers Squibb Research And Development
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Bioorg Med Chem Lett 17: 6539-45 (2007)
Amgen
2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2.
Bioorg Med Chem Lett 17: 6467-71 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.
Eur J Med Chem 43: 1222-9 (2008)
Universit£
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
Bioorg Med Chem 16: 362-73 (2008)
Universit£
Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.
Bioorg Med Chem 16: 530-5 (2008)
Yonsei University
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Bioorg Med Chem Lett 17: 6525-8 (2007)
Pfizer
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Bioorg Med Chem Lett 17: 6593-601 (2007)
Abbott Laboratories
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.
Bioorg Med Chem Lett 17: 6516-20 (2007)
Institute
A phosphorylated prodrug for the inhibition of Pin1.
Bioorg Med Chem Lett 17: 6615-8 (2007)
Virginia Tech
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.
Bioorg Med Chem Lett 17: 6529-34 (2007)
Pfizer
Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.
J Nat Prod 70: 1611-5 (2007)
University Of ZüRich
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.
Bioorg Med Chem 16: 336-53 (2008)
Universit£
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.
Bioorg Med Chem Lett 17: 6567-71 (2007)
The Institute Of Cancer Research
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.
Bioorg Med Chem Lett 17: 6489-92 (2007)
Johnson & Johnson Pharmaceutical Research & Development
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.
Bioorg Med Chem Lett 17: 6493-8 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Bioorg Med Chem Lett 17: 6481-8 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 17: 6546-52 (2007)
Neurocrine Biosciences
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.
J Biol Chem 282: 36829-36 (2007)
Bristol-Myers Squibb Research And Development
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors.
Bioorg Med Chem Lett 17: 6499-504 (2007)
Abbott Laboratories
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
Bioorg Med Chem Lett 17: 6572-5 (2007)
Emd-Serono Research Institute
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 17: 6511-5 (2007)
Merck Research Laboratories
2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors.
Bioorg Med Chem Lett 17: 6579-83 (2007)
Heriot-Watt University
3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b.
Bioorg Med Chem Lett 17: 6619-22 (2007)
Arena Pharmaceuticals
Design, synthesis, structure-selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
J Med Chem 50: 5425-38 (2007)
Nagoya City University
Synthesis, structure-activity relationship and in vivo antiinflammatory efficacy of substituted dipiperidines as CCR2 antagonists.
J Med Chem 50: 5561-3 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.
J Med Chem 50: 5493-508 (2007)
Neuroscience Research
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).
J Med Chem 50: 5564-7 (2007)
Merck Research Laboratories
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
J Med Chem 50: 5550-3 (2007)
Schering-Plough Research Institute
Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice.
J Med Chem 50: 5579-88 (2007)
Università
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.
J Med Chem 50: 5676-84 (2007)
Universit£
Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations.
J Med Chem 50: 5790-5806 (2007)
Cnrs
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
J Med Chem 50: 5528-32 (2007)
University Of Arizona Tucson
A small-molecule therapeutic lead for Huntington's disease: preclinical pharmacology and efficacy of C2-8 in the R6/2 transgenic mouse.
Proc Natl Acad Sci U S A 104: 16685-9 (2007)
Harvard Medical School
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
J Med Chem 50: 5824-32 (2007)
The Johns Hopkins University
De novo discovery of serotonin N-acetyltransferase inhibitors.
J Med Chem 50: 5330-8 (2007)
Johns Hopkins School Of Medicine
Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection.
Antimicrob Agents Chemother 51: 4324-8 (2007)
Tulane University School Of Medicine
ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism.
Nat Chem Biol 3: 722-6 (2007)
Glaxosmithkline
Profiling the enzymatic properties and inhibition of human complement factor B.
J Biol Chem 282: 34809-16 (2007)
University Of Queensland
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.
Bioorg Med Chem Lett 17: 6633-7 (2007)
Amgen
The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies.
Bioorg Med Chem 16: 422-7 (2008)
Neurocrine Biosciences
Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940.
Bioorg Med Chem 16: 322-35 (2008)
Clemson University
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 17: 6056-61 (2007)
Amgen
Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.
Bioorg Med Chem Lett 17: 6079-85 (2007)
Pfizer
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
J Med Chem 50: 5439-48 (2007)
Abbott Laboratories
Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
J Med Chem 50: 5249-52 (2007)
Neurocrine Biosciences
Inhibitors of the Interaction of a Thyroid Hormone Receptor and Coactivators: Preliminary Structure-Activity Relationships.
J Med Chem 50: 5269-5280 (2007)
St. Jude Research Hospital
Interactions of hepatitis B core antigen and peptide inhibitors.
J Med Chem 50: 5620-6 (2007)
Universiti Putra Malaysia
Target specific virtual screening: optimization of an estrogen receptor screening platform.
J Med Chem 50: 5301-10 (2007)
Trinity College
Synthesis and structure-activity relationship for a novel class of potent and selective carbamate-based inhibitors of hormone selective lipase with acute in vivo antilipolytic effects.
J Med Chem 50: 5449-56 (2007)
Novo Nordisk
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
J Med Chem 50: 5403-11 (2007)
Sapienza University Of Rome
CYP2C9 structure-metabolism relationships: substrates, inhibitors, and metabolites.
J Med Chem 50: 5382-91 (2007)
Astrazeneca R&D MöLndal
Structures of Human Monoamine Oxidase B Complexes with Selective Noncovalent Inhibitors: Safinamide and Coumarin Analogs.
J Med Chem 50: 5848-5852 (2007)
University Of Pavia
Pharmacomodulations around the 4-oxo-1,4-dihydroquinoline-3-carboxamides, a class of potent CB2-selective cannabinoid receptor ligands: consequences in receptor affinity and functionality.
J Med Chem 50: 5471-84 (2007)
Université
Small molecule inhibitors of integrin alpha2beta1.
J Med Chem 50: 5457-62 (2007)
University Of Pennsylvania
Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa.
J Med Chem 50: 5339-56 (2007)
Bristol-Myers Squibb
A surface on the androgen receptor that allosterically regulates coactivator binding.
Proc Natl Acad Sci U S A 104: 16074-9 (2007)
University Of California
Potent oxindole based human beta3 adrenergic receptor agonists.
Bioorg Med Chem Lett 17: 6270-3 (2007)
Eli Lilly
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.
Bioorg Med Chem Lett 17: 6378-82 (2007)
Scripps Florida
Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.
Bioorg Med Chem Lett 17: 6066-9 (2007)
Glaxosmithkline
Substituted 2-pyrrolinone inhibitors of HIV-1 integrase.
Bioorg Med Chem Lett 17: 6155-9 (2007)
University Of Southern California
Novel scaffold for cathepsin K inhibitors.
Bioorg Med Chem Lett 17: 6096-100 (2007)
Novartis Institutes For Biomedical Research
Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides.
Bioorg Med Chem Lett 17: 6151-4 (2007)
Bayer Healthcare
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
J Med Chem 50: 5412-24 (2007)
Universit£
Synthesis and monoamine oxidase inhibitory activity of new pyridazine-, pyrimidine- and 1,2,4-triazine-containing tricyclic derivatives.
J Med Chem 50: 5364-71 (2007)
University Of Bari
Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth.
J Med Chem 50: 5281-92 (2007)
University Of Gent
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Bioorg Med Chem 16: 390-9 (2008)
University Of Iowa
Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.
Bioorg Med Chem Lett 17: 6212-5 (2007)
Pedagogical University
Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum.
Bioorg Med Chem 15: 7803-8 (2007)
Hoshi University
Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.
Bioorg Med Chem Lett 17: 6070-4 (2007)
Johnson And Johnson Pharmaceutical Research And Development
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett 17: 6234-8 (2007)
Korea Research Institute Of Bioscience And Biotechnology
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.
Bioorg Med Chem Lett 17: 6111-5 (2007)
Holden Laboratories
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.
Bioorg Med Chem Lett 17: 6220-3 (2007)
Schering-Plough Research Institute
Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Bioorg Med Chem Lett 17: 6123-8 (2007)
Johnson & Johnson Pharmaceutical Research And Development
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
Bioorg Med Chem 16: 457-73 (2008)
Tokyo Medical And Dental University
Estrogen receptor dependent inhibitors of NF-kappaB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: pathway selective inhibitors of NF-kappaB, a potential treatment for rheumatoid arthritis.
J Med Chem 50: 5245-8 (2007)
Wyeth Research
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.
J Med Chem 50: 5311-23 (2007)
Cnrs
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.
Bioorg Med Chem 15: 7576-80 (2007)
Purdue University
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems.
Bioorg Med Chem 15: 7581-9 (2007)
Università
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.
Bioorg Med Chem 16: 437-45 (2008)
Graduate School Of Life Science And Systems Engineering
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Bioorg Med Chem Lett 17: 6280-5 (2007)
Merck Research Laboratories
Rational design, structure, and biological evaluation of cyclic peptides mimicking the vascular endothelial growth factor.
J Med Chem 50: 5135-46 (2007)
Université
Lateral compartmentalization of T cell receptor versus CD45 by galectin-N-glycan binding and microfilaments coordinate basal and activation signaling.
J Biol Chem 282: 35361-72 (2007)
University Of California
Three-dimensional structure of the EphB2 receptor in complex with an antagonistic peptide reveals a novel mode of inhibition.
J Biol Chem 282: 36505-13 (2007)
The Scripps Research Institute
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
Bioorg Med Chem Lett 17: 6188-91 (2007)
Pfizer
Inhibition of human dimethylarginine dimethylaminohydrolase-1 by S-nitroso-L-homocysteine and hydrogen peroxide. Analysis, quantification, and implications for hyperhomocysteinemia.
J Biol Chem 282: 34684-92 (2007)
University Of Texas
1,3-disubstituted ureas functionalized with ether groups are potent inhibitors of the soluble epoxide hydrolase with improved pharmacokinetic properties.
J Med Chem 50: 5217-26 (2007)
Department Of Entomology And University Of California Davis Cancer Center
Phenylimidazole derivatives as specific inhibitors of bacterial enoyl-acyl carrier protein reductase FabK.
Bioorg Med Chem 15: 7325-36 (2007)
Meiji Seika Kaisha
Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.
Bioorg Med Chem Lett 17: 6160-3 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of 5-HT6 receptor ligands based on virtual HTS.
Bioorg Med Chem Lett 17: 6224-9 (2007)
4Sc
Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.
Bioorg Med Chem Lett 17: 6261-5 (2007)
Université
New functional assay of P-glycoprotein activity using Hoechst 33342.
Bioorg Med Chem 15: 7470-9 (2007)
University Of Bonn
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 6290-4 (2007)
Schering-Plough Research Institute
Androstene-3,5-dienes as ER-beta selective SERMs.
Bioorg Med Chem Lett 17: 6295-8 (2007)
Merck Research Laboratories
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.
Bioorg Med Chem 15: 7626-37 (2007)
Universit£
Facile one-pot synthesis of thio and selenourea derivatives: a new class of potent urease inhibitors.
Bioorg Med Chem Lett 17: 6387-91 (2007)
Institute Of Science
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Bioorg Med Chem Lett 17: 6172-7 (2007)
Merck Research Laboratories
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids.
Bioorg Med Chem Lett 17: 6178-82 (2007)
Epicept
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.
Bioorg Med Chem Lett 17: 6373-7 (2007)
Development Center For Biotechnology
2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.
Bioorg Med Chem Lett 17: 6266-9 (2007)
Johnson & Johnson
Unique spirocyclopiperazinium salt III: further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics.
Bioorg Med Chem Lett 17: 6245-9 (2007)
Peking University
Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: derivatives of irbesartan key intermediate.
Bioorg Med Chem 15: 7391-8 (2007)
University Of Mysore
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.
Bioorg Med Chem Lett 17: 6250-6 (2007)
Pfizer
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
J Med Chem 50: 5176-82 (2007)
University Of Bath
Macrolactins O-R, glycosylated 24-membered lactones from Bacillus sp. AH159-1.
J Nat Prod 70: 1632-5 (2007)
Korea Research Institute Of Bioscience And Biotechnology
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.
J Med Chem 50: 5253-6 (2007)
Pfizer
Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.
J Med Chem 50: 5049-52 (2007)
Ligand Pharmaceuticals
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
J Med Chem 50: 5202-16 (2007)
Bayer Pharmaceuticals
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.
Bioorg Med Chem Lett 17: 5886-93 (2007)
Glaxosmithkline
N-Alkylidenearylcarboxamides as new potent and selective CB(2) cannabinoid receptor agonists with good oral bioavailability.
Bioorg Med Chem Lett 17: 6299-304 (2007)
Taisho Pharmaceutical
Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
Bioorg Med Chem Lett 17: 6305-10 (2007)
Molecular Cancer Research Center
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
Bioorg Med Chem Lett 17: 6183-7 (2007)
Astrazeneca R&D Montreal
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.
Bioorg Med Chem Lett 17: 6206-11 (2007)
Novartis Institutes For Biomedical Research
Rynaxypyr: a new insecticidal anthranilic diamide that acts as a potent and selective ryanodine receptor activator.
Bioorg Med Chem Lett 17: 6274-9 (2007)
Fmc Stine Research Center
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.
J Nat Prod 70: 1570-7 (2007)
Chinese Academy Of Sciences
Novel C2-purine position analogs of nitrobenzylmercaptopurine riboside as human equilibrative nucleoside transporter 1 inhibitors.
Bioorg Med Chem 15: 7726-37 (2007)
University Of Tennessee Health Sciences Center
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.
Bioorg Med Chem 15: 7830-9 (2007)
Graduate School Of Life Science And Systems Engineering
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
J Med Chem 50: 5103-8 (2007)
Solvay Pharma
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.
J Med Chem 50: 5090-102 (2007)
University Of Auckland
Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.
J Med Chem 50: 5161-7 (2007)
Elan Pharmaceuticals
Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.
Proc Natl Acad Sci U S A 104: 15490-5 (2007)
Metabasis Therapeutics
Biochemical Characterization of SFC-1, a class A carbapenem-hydrolyzing beta-lactamase.
Antimicrob Agents Chemother 51: 4512-4 (2007)
University Of Aveiro
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
Antimicrob Agents Chemother 51: 4356-60 (2007)
National Science And Technology Development Agency
In vitro efficacy of new antifolates against trimethoprim-resistant Bacillus anthracis.
Antimicrob Agents Chemother 51: 4447-52 (2007)
Oklahoma State University
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
J Biol Chem 282: 33052-63 (2007)
University Of California San Francisco
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.
Bioorg Med Chem 15: 7399-407 (2007)
Peking University
Additional level of information about complex interaction between non-nucleoside inhibitor and HIV-1 reverse transcriptase using biosensor-based thermodynamic analysis.
Bioorg Med Chem 15: 7344-54 (2007)
Uppsala University
Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity.
Bioorg Med Chem 15: 7480-93 (2007)
Instituto De QuíMica MéDica
Validation of an automated procedure for the prediction of relative free energies of binding on a set of aldose reductase inhibitors.
Bioorg Med Chem 15: 7865-77 (2007)
Università
Two new phenylpiperazines with atypical antipsychotic potential.
Bioorg Med Chem Lett 17: 5749-53 (2007)
Institute For Biological Research
Synthesis of novel anilinoquinolines as c-fms inhibitors.
Bioorg Med Chem Lett 17: 6257-60 (2007)
Glaxosmithkline
Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors.
Eur J Med Chem 43: 1248-60 (2008)
The University Of Manchester
4-thiazolidinone--a biologically active scaffold.
Eur J Med Chem 43: 897-905 (2008)
Northern India Engineering College
The molecular pruning of a phosphoramidate peptidomimetic inhibitor of prostate-specific membrane antigen.
Bioorg Med Chem 15: 7434-43 (2007)
San Francisco State University
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.
Bioorg Med Chem 15: 7677-87 (2007)
University Of Auckland
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.
Bioorg Med Chem 15: 7361-7 (2007)
Central Drug Research Institute
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.
Bioorg Med Chem Lett 17: 6003-8 (2007)
Amgen
Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Bioorg Med Chem Lett 17: 6326-9 (2007)
Astrazeneca
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Bioorg Med Chem Lett 17: 5853-7 (2007)
Merck Research Laboratories
Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.
Bioorg Med Chem Lett 17: 5863-7 (2007)
Mitsubishi Pharma
Amino-caprolactam derivatives as gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 5790-5 (2007)
Bristol-Myers Squibb Research And Development
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.
Eur J Med Chem 43: 1276-96 (2008)
University Of Auckland
Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds.
Bioorg Med Chem 15: 7380-90 (2007)
Università
Structure-activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2.
Bioorg Med Chem 15: 7408-25 (2007)
Universidad De Santiago De Chile
Synthesis and biological evaluation of phenyl piperidine derivatives as CCR2 antagonists.
Bioorg Med Chem Lett 17: 5964-8 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of potent T-type calcium channel blocker.
Bioorg Med Chem Lett 17: 5740-3 (2007)
Kyung Hee University
High dopamine transporter selectivity can be displayed by remarkably simple non-nitrogen containing inhibitors.
Bioorg Med Chem Lett 17: 6019-25 (2007)
University Of Aarhus
Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.
Bioorg Med Chem Lett 17: 5928-33 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 5918-23 (2007)
F. Hoffmann-La Roche
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.
J Med Chem 50: 5076-89 (2007)
Glaxosmithkline
Synthesis and radioligand binding studies of bis-isoquinolinium derivatives as small conductance Ca(2+)-activated K(+) channel blockers.
J Med Chem 50: 5070-5 (2007)
University Of Li£Ge
Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase.
J Biol Chem 282: 32549-60 (2007)
Lund University
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.
J Biol Chem 282: 34663-71 (2007)
Merck Research Laboratories
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.
Bioorg Med Chem Lett 17: 5754-7 (2007)
Rti International
Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors.
Bioorg Med Chem Lett 17: 5876-80 (2007)
Purdue University
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.
Bioorg Med Chem Lett 17: 5952-8 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
Bioorg Med Chem Lett 17: 5796-800 (2007)
Wyeth Research
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.
J Med Chem 50: 5147-60 (2007)
Schering-Plough Research Institute
Brunneins A-C, beta-carboline alkaloids from Cortinarius brunneus.
J Nat Prod 70: 1529-31 (2007)
Institute Of Plant Biochemistry
Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents.
Bioorg Med Chem 15: 7809-29 (2007)
Institute Of Pharmaceutical Industry
Myricetin inhibits Escherichia coli DnaB helicase but not primase.
Bioorg Med Chem 15: 7203-8 (2007)
University Of Nebraska-Lincoln
A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
Bioorg Med Chem 15: 6876-81 (2007)
University Of Ferrara
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.
Bioorg Med Chem Lett 17: 5806-11 (2007)
Merck Research Laboratories
Inactivation of soybean sterol 24-C-methyltransferase by elongated sterol side chains at C26.
Bioorg Med Chem Lett 17: 5902-6 (2007)
Texas Tech University
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Bioorg Med Chem Lett 17: 5825-30 (2007)
Amgen
The selectivity of protein kinase inhibitors: a further update.
Biochem J 408: 297-315 (2007)
University Of Dundee
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
J Med Chem 50: 4882-97 (2007)
University Of Bologna
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.
J Med Chem 50: 4789-92 (2007)
James Black Foundation
4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization.
J Med Chem 50: 5043-7 (2007)
Università
N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.
J Med Chem 50: 4928-38 (2007)
Montana State University
Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands.
J Med Chem 50: 4993-5002 (2007)
University Of Florence
Biological evaluation, structure-activity relationships, and three-dimensional quantitative structure-activity relationship studies of dihydro-beta-agarofuran sesquiterpenes as modulators of P-glycoprotein-dependent multidrug resistance.
J Med Chem 50: 4808-17 (2007)
Instituto Universitario De Bio-Organica Antonio Gonzalez
Discovery of a new series of potent and selective linear tachykinin NK2 receptor antagonists.
J Med Chem 50: 4793-807 (2007)
Menarini Ricerche
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
J Med Chem 50: 4976-85 (2007)
Institute Genomics Functional (Igf)
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.
J Biol Chem 282: 33295-304 (2007)
Wyeth Research
Accumulation of glucosylceramide in murine testis, caused by inhibition of beta-glucosidase 2: implications for spermatogenesis.
J Biol Chem 282: 32655-64 (2007)
University Of Oxford
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
Antimicrob Agents Chemother 51: 4133-40 (2007)
Veterans Affairs Medical Center
Molecular and biochemical characterization of the chromosome-encoded class A beta-lactamase BCL-1 from Bacillus clausii.
Antimicrob Agents Chemother 51: 4009-14 (2007)
H�Pital De Bic�Tre
Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray crystallography.
Antimicrob Agents Chemother 51: 3915-23 (2007)
University Of California San Francisco
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.
Bioorg Med Chem 15: 7184-202 (2007)
LinköPing University
Is adamantane a suitable substituent to pre-organize the acid orientation in E-selectin antagonists?
Bioorg Med Chem 16: 1046-56 (2008)
University Of Basel
Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.
Bioorg Med Chem Lett 17: 5924-7 (2007)
University Of Southern Denmark
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
J Med Chem 50: 5003-11 (2007)
Universit£
Pyrido[1,2-a]pyrimidin-4-one derivatives as a novel class of selective aldose reductase inhibitors exhibiting antioxidant activity.
J Med Chem 50: 4917-27 (2007)
Università
Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase.
J Med Chem 50: 4845-53 (2007)
University Of Queensland
Benzochromenones from the marine crinoid Comantheria rotula inhibit hypoxia-inducible factor-1 (HIF-1) in cell-based reporter assays and differentially suppress the growth of certain tumor cell lines.
J Nat Prod 70: 1462-6 (2007)
University Of Mississippi
Novel, potent THC/anandamide (hybrid) analogs.
Bioorg Med Chem 15: 7850-64 (2007)
Organix
Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.
Bioorg Med Chem 15: 6956-74 (2007)
Jagiellonian University Medical College
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.
Bioorg Med Chem 15: 7248-57 (2007)
Friedrich-Alexander University
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors.
Bioorg Med Chem Lett 17: 5465-71 (2007)
Universit£
Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor.
Bioorg Med Chem Lett 17: 5472-8 (2007)
Pfizer
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.
Bioorg Med Chem Lett 17: 5944-51 (2007)
Abbott Laboratories
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.
Bioorg Med Chem Lett 17: 5812-8 (2007)
Targegen
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Bioorg Med Chem Lett 17: 5831-5 (2007)
Merck Research Laboratories
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Bioorg Med Chem Lett 17: 5978-82 (2007)
Tanabe Research Laboratories Usa
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Bioorg Med Chem Lett 17: 6013-8 (2007)
Astrazeneca
N(4)-Phenyl modifications of N(2)-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
Bioorg Med Chem Lett 17: 5783-9 (2007)
Nih
Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors.
Bioorg Med Chem Lett 17: 5995-9 (2007)
Entremed
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
Bioorg Med Chem Lett 17: 5934-9 (2007)
Merck Research Laboratories
Synthesis of poison-frog alkaloids 233A, 235U, and 251AA and their inhibitory effects on neuronal nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 17: 5872-5 (2007)
University Of Toyama
(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.
Bioorg Med Chem Lett 17: 5983-8 (2007)
Pfizer
Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.
Bioorg Med Chem Lett 17: 5940-3 (2007)
University Of Texas Medical Branch
Conformationally constrained analogues of 2-arachidonoylglycerol.
Bioorg Med Chem Lett 17: 5959-63 (2007)
Northeastern University
Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.
Bioorg Med Chem Lett 17: 5768-71 (2007)
Kobe Gakuin University
5'-halogenated analogs of oxymorphindole.
Bioorg Med Chem Lett 17: 5916-7 (2007)
University Of Maryland
Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides.
Bioorg Med Chem 15: 7229-36 (2007)
Kochi Medical School
Discovery of platelet-type 12-human lipoxygenase selective inhibitors by high-throughput screening of structurally diverse libraries.
Bioorg Med Chem 15: 6900-8 (2007)
University Of California
Inhibitory effect of synthetic C-C biflavones on various phospholipase A(2)s activity.
Bioorg Med Chem 15: 7138-43 (2007)
Yeungnam University
Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.
Bioorg Med Chem 15: 7258-73 (2007)
Johann Wolfgang Goethe University
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
Bioorg Med Chem Lett 17: 5514-7 (2007)
Glaxosmithkline
On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition.
Bioorg Med Chem Lett 17: 5590-4 (2007)
Université
Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.
Bioorg Med Chem 15: 7166-83 (2007)
Uppsala University
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
Bioorg Med Chem 15: 7116-25 (2007)
Polish Academy Of Sciences
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
J Med Chem 50: 4953-75 (2007)
Irbm-Mrl
Structural Modification of the P2' Position of 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The Discovery of Aliskiren, a Potent Nonpeptide Human Renin Inhibitor Active after Once Daily Dosing in Marmosets.
J Med Chem 50: 4832-44 (2007)
Novartis Pharmaceuticals
Novel 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamide Transition State Peptidomimetics Are Potent and Orally Active Inhibitors of Human Renin.
J Med Chem 50: 4818-31 (2007)
Novartis Pharmaceuticals
Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase.
J Med Chem 50: 4909-16 (2007)
University Of Bari
Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2-thione derivatives with carbonic anhydrase inhibitory activity.
Bioorg Med Chem 15: 6975-84 (2007)
Assiut University
Pyrazole-based cathepsin S inhibitors with improved cellular potency.
Bioorg Med Chem Lett 17: 5525-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality.
Bioorg Med Chem Lett 17: 5614-9 (2007)
University Of Minnesota
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 17: 5595-9 (2007)
Merck Research Laboratories
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
Bioorg Med Chem Lett 17: 5704-8 (2007)
Corcept Therapeutics
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 17: 5610-3 (2007)
Neurocrine Biosciences
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
Bioorg Med Chem Lett 17: 5634-7 (2007)
Shaheed Beheshti University Of Medical Sciences
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Bioorg Med Chem Lett 17: 5638-42 (2007)
Pfizer
3D-QSAR studies of triazafluorenone inhibitors of metabotropic glutamate receptor subtype 1.
Eur J Med Chem 43: 1025-34 (2008)
Biocampus
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.
J Nat Prod 70: 1458-61 (2007)
Chinese Academy Of Sciences
5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).
Bioorg Med Chem Lett 17: 5630-3 (2007)
Wyeth Research
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 17: 5671-6 (2007)
Merck Research Laboratories
Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis.
Bioorg Med Chem Lett 17: 5543-7 (2007)
Schering-Plough Research Institute
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.
Bioorg Med Chem Lett 17: 5573-6 (2007)
Chugai Pharmaceutical
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.
Bioorg Med Chem Lett 17: 5600-4 (2007)
Eli Lilly
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Bioorg Med Chem Lett 17: 5989-94 (2007)
Merck Research Laboratories
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
Bioorg Med Chem Lett 17: 5563-6 (2007)
Eli Lilly
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Bioorg Med Chem Lett 17: 5577-81 (2007)
Astellas Pharma
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Bioorg Med Chem Lett 17: 5620-3 (2007)
Arena Pharmaceuticals
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
J Med Chem 50: 5024-33 (2007)
Pierre Fabre Research Center
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
J Med Chem 50: 4854-67 (2007)
Purdue University
Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.
Bioorg Med Chem Lett 17: 5665-70 (2007)
Abbott Laboratories
Discovery of novel and orally active NR2B-selective N-methyl-D-aspartate (NMDA) antagonists, pyridinol derivatives with reduced HERG binding affinity.
Bioorg Med Chem Lett 17: 5533-6 (2007)
Pfizer
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
Bioorg Med Chem Lett 17: 5720-3 (2007)
Merck
Synthesis and characterization of a pegylated derivative of 3-(1,2,3,6-tetrahydro-pyridin-4yl)-1H-indole (IDT199): a high affinity SERT ligand for conjugation to quantum dots.
Bioorg Med Chem Lett 17: 5656-60 (2007)
Vanderbilt University
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.
Bioorg Med Chem Lett 17: 5647-51 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.
Bioorg Med Chem Lett 17: 5693-7 (2007)
Pfizer
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 17: 5677-82 (2007)
Merck Research Laboratories
Synthesis and biological evaluation of a C5-biphenyl thiolactomycin library.
Bioorg Med Chem Lett 17: 5643-6 (2007)
University Of Birmingham
Novel anti-infection agents: small-molecule inhibitors of bacterial transcription factors.
Bioorg Med Chem Lett 17: 5652-5 (2007)
Paratek Pharmaceuticals
Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation.
Bioorg Med Chem Lett 17: 5537-42 (2007)
Pfizer
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
Bioorg Med Chem Lett 17: 5558-62 (2007)
Pfizer
Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli.
Bioorg Med Chem 15: 6834-45 (2007)
University Of London
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.
Bioorg Med Chem 15: 6819-29 (2007)
Johannes Gutenberg University
Dual serotonin transporter inhibitor/histamine H3 antagonists: development of rigidified H3 pharmacophores.
Bioorg Med Chem Lett 17: 5325-9 (2007)
Johnson & Johnson Pharmaceutical Research And Development
A refined agonist pharmacophore for protease activated receptor 2.
Bioorg Med Chem Lett 17: 5552-7 (2007)
University Of Queensland
Nucleation of an allosteric response via ligand-induced loop folding.
J Mol Biol 373: 96-111 (2007)
University Of Maryland College Park
Novel (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic ester prodrugs possessing a diazen-1-ium-1,2-diolate moiety: design, synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
Bioorg Med Chem 15: 6796-801 (2007)
University Of Alberta
Thiazole-diamides as potent gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 5518-22 (2007)
Pfizer
Pyrazole inhibitors of HMG-CoA reductase: An attempt to dramatically reduce synthetic complexity through minimal analog re-design.
Bioorg Med Chem Lett 17: 5567-72 (2007)
Pfizer
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.
Bioorg Med Chem Lett 17: 5529-32 (2007)
Pfizer
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Bioorg Med Chem Lett 17: 5686-9 (2007)
Crystalgenomics
Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase.
J Med Chem 50: 5012-23 (2007)
Universidad Complutense
Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening.
Bioorg Med Chem 15: 6810-8 (2007)
Waseda University
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 17: 5390-5 (2007)
Merck Research Laboratories
Thiophene substituted acylguanidines as BACE1 inhibitors.
Bioorg Med Chem Lett 17: 5353-6 (2007)
Wyeth Research
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 5330-5 (2007)
Schering-Plough Research Institute
The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.
Bioorg Med Chem Lett 17: 5300-9 (2007)
Merck Research Laboratories
Influence of conformation on GRIND-based three-dimensional quantitative structure-activity relationship (3D-QSAR).
J Med Chem 50: 5039-42 (2007)
Universit£
2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.
Bioorg Med Chem Lett 17: 5357-60 (2007)
Inha University
Novel ATP-competitive kinesin spindle protein inhibitors.
J Med Chem 50: 4939-52 (2007)
Glaxosmithkline
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.
J Med Chem 50: 4630-41 (2007)
Universit£
A Ser678Pro substitution in Fks1p confers resistance to echinocandin drugs in Aspergillus fumigatus.
Antimicrob Agents Chemother 51: 4174-6 (2007)
Umdnj-New Jersey Medical School
Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.
J Biol Chem 282: 30699-706 (2007)
University Of Utah
Inhibition of the Mycobacterium tuberculosis enoyl acyl carrier protein reductase InhA by arylamides.
Bioorg Med Chem 15: 6649-58 (2007)
Incyte
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Bioorg Med Chem Lett 17: 5310-5 (2007)
Merck Research Laboratories
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
Bioorg Med Chem Lett 17: 5428-31 (2007)
Darmstadt University Of Technology
Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
Bioorg Med Chem Lett 17: 5396-9 (2007)
Pfizer
Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide.
J Med Chem 50: 4669-80 (2007)
Université
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
J Med Chem 50: 4616-29 (2007)
University Of Copenhagen
Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.
J Med Chem 50: 4868-81 (2007)
Astrazeneca Discovery
L-(+)-2-Amino-4-thiophosphonobutyric acid (L-thioAP4), a new potent agonist of group III metabotropic glutamate receptors: increased distal acidity affords enhanced potency.
J Med Chem 50: 4656-64 (2007)
Université
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.
J Med Chem 50: 4585-605 (2007)
University Of Washington
Synthesis and structure-affinity relationships of new 4-(6-iodo-H-imidazo[1,2-a]pyridin-2-yl)-N-dimethylbenzeneamine derivatives as ligands for human beta-amyloid plaques.
J Med Chem 50: 4746-58 (2007)
National Institute Of Mental Health
Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile.
Bioorg Med Chem Lett 17: 5340-4 (2007)
Gedeon Richter
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Bioorg Med Chem Lett 17: 5349-52 (2007)
Eli Lilly
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).
Bioorg Med Chem Lett 17: 5455-61 (2007)
Bristol-Myers Squibb
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.
Eur J Med Chem 43: 1008-14 (2008)
Università
Virtual screening application of a model of full-length HIV-1 integrase complexed with viral DNA.
Bioorg Med Chem Lett 17: 5361-5 (2007)
National Cancer Institute
Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists.
Chem Biol Drug Des 70: 268-72 (2007)
Pfizer
Crystal structure of the T315I mutant of AbI kinase.
Chem Biol Drug Des 70: 171-81 (2007)
Ariad Pharmaceuticals
Carbocyclic 3'-deoxyadenosine-based highly potent bisubstrate-analog inhibitor of basophilic protein kinases.
Bioorg Med Chem Lett 17: 5336-9 (2007)
University Of Tartu
Toward novel HIV-1 integrase binding inhibitors: molecular modeling, synthesis, and biological studies.
Bioorg Med Chem Lett 17: 5370-3 (2007)
Universit£
Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos.
Bioorg Med Chem Lett 17: 5366-9 (2007)
Seoul National University
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.
J Med Chem 50: 4728-45 (2007)
Wyeth Research
Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers.
J Biol Chem 282: 30062-9 (2007)
Université
Exploration of physicochemical properties and molecular modelling studies of 2-sulfonyl-phenyl-3-phenyl-indole analogs as cyclooxygenase-2 inhibitors.
Eur J Med Chem 43: 1297-303 (2008)
Institute Of Technology And Science
Phenylimidazole derivatives of 4-pyridone as dual inhibitors of bacterial enoyl-acyl carrier protein reductases FabI and FabK.
J Med Chem 50: 4710-20 (2007)
Meiji Seika Kaisha
Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
J Med Chem 50: 4648-55 (2007)
Universit£
Novel small-molecule inhibitors of transmissible gastroenteritis virus.
Antimicrob Agents Chemother 51: 3924-31 (2007)
National Health Research Institute
TEM-158 (CMT-9), a new member of the CMT-type extended-spectrum beta-lactamases.
Antimicrob Agents Chemother 51: 4181-3 (2007)
Chu Clermont-Ferrand
Quinuclidine derivatives as potential antiparasitics.
Antimicrob Agents Chemother 51: 4049-61 (2007)
Cardiff University
Correlation of carboxylic acid pKa to protein binding and antibacterial activity of a novel class of bacterial translation inhibitors.
Bioorg Med Chem Lett 17: 5479-82 (2007)
Pharmacia
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.
Bioorg Med Chem Lett 17: 5384-9 (2007)
Amgen
Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.
J Nat Prod 70: 1397-405 (2007)
University Of Mississippi
Selectivity criterion for pyrazolo[3,4-b]pyrid[az]ine derivatives as GSK-3 inhibitors: CoMFA and molecular docking studies.
Eur J Med Chem 43: 949-57 (2008)
National Institute Of Pharmaceutical Education And Research
QSAR studies on benzoylaminobenzoic acid derivatives as inhibitors of beta-ketoacyl-acyl carrier protein synthase III.
Eur J Med Chem 43: 1071-80 (2008)
Shri G.S. Institute Of Technology And Science
Pyrimidine benzamide-based thrombopoietin receptor agonists.
Bioorg Med Chem Lett 17: 5447-54 (2007)
Pfizer
Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.
Eur J Med Chem 43: 830-8 (2008)
University College Of Pharmaceutical Sciences
Schiff base transition metal complexes as novel inhibitors of xanthine oxidase.
Eur J Med Chem 43: 862-71 (2008)
Nanjing University
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
J Med Chem 50: 4699-709 (2007)
Ligand Pharmaceuticals
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.
J Med Chem 50: 4681-98 (2007)
Wyeth Research
Synthesis and in vivo evaluation of fluorine-18 and iodine-123 labeled 2beta-carbo(2-fluoroethoxy)-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane as a candidate serotonin transporter imaging agent.
J Med Chem 50: 4553-60 (2007)
Emory University
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
Bioorg Med Chem Lett 17: 5442-6 (2007)
Ligand Pharmaceuticals
Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.
J Biol Chem 282: 29803-11 (2007)
University Of Washington
Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter.
J Biol Chem 282: 29441-7 (2007)
Yale University
Targeting of the Brucella suis virulence factor histidinol dehydrogenase by histidinol analogues results in inhibition of intramacrophagic multiplication of the pathogen.
Antimicrob Agents Chemother 51: 3752-5 (2007)
University Of Montpellier
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
Eur J Med Chem 43: 621-32 (2008)
Sapienza University Of Rome
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.
Bioorg Med Chem 15: 6574-95 (2007)
Amgen
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.
J Med Chem 50: 4509-15 (2007)
Georgia State University
Design and Synthesis of HIV-1 Protease Inhibitors Incorporating Oxazolidinones as P2/P2' Ligands in Pseudosymmetric Dipeptide Isosteres.
J Med Chem 50: 4316-28 (2007)
University Of Massachusetts Medical School
Conformation-activity relationship of neuropeptide S and some structural mutants: helicity affects their interaction with the receptor.
J Med Chem 50: 4501-8 (2007)
Istituto Di Chimica Biomolecolare
3,17-disubstituted 2-alkylestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anticancer activity.
J Med Chem 50: 4431-43 (2007)
University Of Bath
Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.
J Med Chem 50: 4351-4373 (2007)
Amgen
Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.
J Med Chem 50: 4471-81 (2007)
University Of Southern California
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.
J Med Chem 50: 4374-81 (2007)
University Of Tennessee At Knoxville
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
Proc Natl Acad Sci U S A 104: 13827-32 (2007)
University Of Utah
Synthetic tyrosyl gallate derivatives as potent melanin formation inhibitors.
Bioorg Med Chem Lett 17: 5462-4 (2007)
Amorepacific
New amido derivatives as potential BKCa potassium channel activators. XI.
Eur J Med Chem 43: 792-9 (2008)
Universit£
Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.
Bioorg Med Chem 15: 6535-48 (2007)
Inha University
Identification of dissociated non-steroidal glucocorticoid receptor agonists.
Bioorg Med Chem Lett 17: 5025-31 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.
Bioorg Med Chem Lett 17: 5432-6 (2007)
Merck Research Laboratories
Aldehyde dehydrogenase inhibitors: alpha,beta-acetylenic N-substituted aminothiolesters are reversible growth inhibitors of normal epithelial but irreversible apoptogens for cancer epithelial cells from human prostate in culture.
Eur J Med Chem 43: 906-16 (2008)
Claude Bernard University Lyon 1
Synthesis of N-aryl-5-amino-4-cyanopyrazole derivatives as potent xanthine oxidase inhibitors.
Eur J Med Chem 43: 771-80 (2008)
Universidade Do Minho
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement.
Eur J Med Chem 43: 966-72 (2008)
University Of Montpellier
2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.
J Med Chem 50: 4405-18 (2007)
University Of Regensburg
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.
J Med Chem 50: 4516-27 (2007)
University Of Dublin
LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake.
Science 317: 1390-3 (2007)
New York University School Of Medicine
Towards predictive inhibitor design for the EGFR autophosphorylation activity.
Eur J Med Chem 43: 781-91 (2008)
Korea Institute Of Science And Technology
Dual acting antioxidant A1 adenosine receptor agonists.
Bioorg Med Chem Lett 17: 5437-41 (2007)
Monash University (Parkville Campus)
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
Bioorg Med Chem Lett 17: 5406-9 (2007)
Abbott Laboratories
Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity.
J Biol Chem 282: 28501-13 (2007)
University WüRzburg
3,3-diphenylpentane skeleton as a steroid skeleton substitute: novel inhibitors of human 5alpha-reductase 1.
Bioorg Med Chem Lett 17: 5414-8 (2007)
The University Of Tokyo
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
J Nat Prod 70: 1278-82 (2007)
The University Of Iowa
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.
J Med Chem 50: 4265-8 (2007)
University Di Perugia
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.
J Med Chem 50: 4279-94 (2007)
Targegen
2-Amino-3,4-dihydroquinazolines as Inhibitors of BACE-1 (beta-Site APP Cleaving Enzyme): Use of Structure Based Design to Convert a Micromolar Hit into a Nanomolar Lead.
J Med Chem 50: 4261-4 (2007)
Johnson & Johnson Pharmaceutical
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.
Proc Natl Acad Sci U S A 104: 13283-8 (2007)
Center For Molecular Medicine Of The Austrian Academy Of Sciences
4-Hydroxynonenal, an endogenous aldehyde, causes pain and neurogenic inflammation through activation of the irritant receptor TRPA1.
Proc Natl Acad Sci U S A 104: 13519-24 (2007)
Florence University
Structure of compstatin in complex with complement component C3c reveals a new mechanism of complement inhibition.
J Biol Chem 282: 29241-7 (2007)
Utrecht University
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Bioorg Med Chem Lett 17: 5150-4 (2007)
Schering-Plough Research Institute
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Bioorg Med Chem 15: 6556-64 (2007)
Wyeth Research
Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.
Bioorg Med Chem 15: 6596-607 (2007)
Woosuk University
Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine.
Bioorg Med Chem 15: 6367-78 (2007)
Dalhousie University
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.
Bioorg Med Chem Lett 17: 5032-5 (2007)
Griffith University
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.
Bioorg Med Chem Lett 17: 5091-5 (2007)
Boehringer Ingelheim Pharmaceuticals
Dopamine/serotonin receptor ligands. 16.(1) Expanding dibenz[d,g]azecines to 11- and 12-membered homologues. Interaction with dopamine D(1)-D(5) receptors.
J Med Chem 50: 4528-33 (2007)
Friedrich-Schiller-UniversitäT Jena
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors.
J Med Chem 50: 4453-70 (2007)
Gsk
Targeting plague virulence factors: a combined machine learning method and multiple conformational virtual screening for the discovery of Yersinia protein kinase A inhibitors.
J Med Chem 50: 3980-3 (2007)
The Rockefeller University
Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers.
J Med Chem 50: 4482-92 (2007)
Paris-Sud University
Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist.
J Med Chem 50: 4543-7 (2007)
Institute Of Science And Technology
Structural and mechanistic basis of penicillin-binding protein inhibition by lactivicins.
Nat Chem Biol 3: 565-9 (2007)
Universit£
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
J Biol Chem 282: 28408-18 (2007)
University Of Minnesota
Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.
J Med Chem 50: 4177-85 (2007)
University Of Copenhagen
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
J Med Chem 50: 4135-46 (2007)
National Institute On Drug Abuse-Intramural Research Program
C1'-cycloalkyl side chain pharmacophore in tetrahydrocannabinols.
J Med Chem 50: 4048-60 (2007)
National Hellenic Research Foundation
Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease.
Proc Natl Acad Sci U S A 104: 13192-7 (2007)
Nih
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
J Med Chem 50: 3883-90 (2007)
Lundbeck Research Usa
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
J Med Chem 50: 3870-82 (2007)
Lundbeck Research Usa
Design, synthesis, and in vitro evaluation of carbamate derivatives of 2-benzoxazolyl- and 2-benzothiazolyl-(3-hydroxyphenyl)-methanones as novel fatty acid amide hydrolase inhibitors.
J Med Chem 50: 4236-42 (2007)
Helsinki University Of Technology
N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.
J Med Chem 50: 4255-9 (2007)
Gnf
4-Substituted trinems as broad spectrum beta-lactamase inhibitors: structure-based design, synthesis, and biological activity.
J Med Chem 50: 4113-21 (2007)
Lek Pharmaceuticals
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
J Med Chem 50: 4061-74 (2007)
Università
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
J Med Chem 50: 4027-37 (2007)
University Of Athens
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
Antimicrob Agents Chemother 51: 3498-504 (2007)
Gilead Sciences
Plasmid-encoded ACC-4, an extended-spectrum cephalosporinase variant from Escherichia coli.
Antimicrob Agents Chemother 51: 3763-7 (2007)
Institute
The phenolic diterpene totarol inhibits multidrug efflux pump activity in Staphylococcus aureus.
Antimicrob Agents Chemother 51: 4480-3 (2007)
University Of London
Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.
Bioorg Med Chem 15: 6425-42 (2007)
Wyeth Research
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.
Bioorg Med Chem Lett 17: 5019-24 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
In vitro PAI-1 inhibitory activity of oxalamide derivatives.
Eur J Med Chem 43: 880-4 (2008)
Zydus Research Centre
Synthesis, Biological Activity, and Crystal Structure of Potent Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase That Retain Activity against Mutant Forms of the Enzyme.
J Med Chem 50: 4003-4015 (2007)
Nci-Fcrdc
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
Bioorg Med Chem Lett 17: 4753-5 (2007)
Wonkwang University
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring.
Bioorg Med Chem Lett 17: 5082-5 (2007)
Eli Lilly
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
J Pharmacol Exp Ther 323: 285-93 (2007)
Abbott Laboratories
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.
Bioorg Med Chem Lett 17: 5175-6 (2007)
University Of Maryland
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.
J Med Chem 50: 4162-76 (2007)
Abbott Laboratories
Discovery and optimization of p38 inhibitors via computer-assisted drug design.
J Med Chem 50: 4016-26 (2007)
Boehringer Ingelheim Pharmaceuticals
New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET.
Bioorg Med Chem Lett 17: 4991-5 (2007)
University Of Tours
Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides.
J Biol Chem 282: 28096-105 (2007)
Michigan State University
Rational design, synthesis, and biological evaluation of progesterone-modified MRI contrast agents.
Chem Biol 14: 824-34 (2007)
Northwestern University
Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases.
Chem Biol 14: 764-74 (2007)
The Johns Hopkins University
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.
Bioorg Med Chem Lett 17: 4761-6 (2007)
University Of Pennsylvania
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.
Bioorg Med Chem Lett 17: 5115-20 (2007)
Bristol-Myers Squibb
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.
Biochemistry 46: 9551-63 (2007)
Abbott Laboratories
Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30.
ACS Chem Biol 2: 536-44 (2007)
University Of New Mexico Health Sciences Center
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
J Med Chem 50: 4147-61 (2007)
University Of Copenhagen
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.
J Med Chem 50: 4250-4 (2007)
University Of Bologna
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
Proc Natl Acad Sci U S A 104: 13432-7 (2007)
University Of California
Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.
Bioorg Med Chem Lett 17: 4808-11 (2007)
Tsukuba Research Institute
Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.
Bioorg Med Chem Lett 17: 4804-7 (2007)
Tsukuba Research Institute
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
J Med Chem 50: 4214-21 (2007)
Universita Degli Studi Di Bari
Biochemical and biophysical characterization of inhibitor binding to caspase-3 reveals induced asymmetry.
Biochemistry 46: 9462-71 (2007)
Wyeth Research
Design of protein membrane interaction inhibitors by virtual ligand screening, proof of concept with the C2 domain of factor V.
Proc Natl Acad Sci U S A 104: 12697-702 (2007)
Maastricht University
(R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1.
J Biol Chem 282: 31542-8 (2007)
Institut De Biologie Et Chimie Des ProtéInes
A novel approach to cyclin-dependent kinase 5/p25 inhibitors: A potential treatment for Alzheimer's disease.
Bioorg Med Chem 15: 6397-406 (2007)
Dr. Reddy'S Laboratories
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bioorg Med Chem Lett 17: 5041-8 (2007)
Bristol-Myers Squibb
Sulfonamide derivatives as new potent and selective CB2 cannabinoid receptor agonists.
Bioorg Med Chem Lett 17: 5133-5 (2007)
Taisho Pharmaceutical
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
Nat Chem Biol 3: 570-5 (2007)
Eisai
Cyclic nucleotide phosphodiesterase type 4 inhibitors: evaluation of pyrazolo[1,5-a]-1,3,5-triazine ring system as an adenine bioisostere.
Eur J Med Chem 43: 816-29 (2008)
Université
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
Cancer Res 67: 6916-24 (2007)
University Hospital Basel
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.
Antimicrob Agents Chemother 51: 4036-43 (2007)
Ambrilia Biopharma
Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase.
Bioorg Med Chem 15: 6463-73 (2007)
Loma Linda University School Of Medicine
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Bioorg Med Chem Lett 17: 5191-8 (2007)
Merck
Dragon method for finding novel tyrosinase inhibitors: Biosilico identification and experimental in vitro assays.
Eur J Med Chem 42: 1370-81 (2007)
Central University Of Las Villas
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.
J Med Chem 50: 3841-50 (2007)
University Of Mississippi
Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors.
J Med Chem 50: 3906-20 (2007)
University Of Tennessee Health Science Center
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
J Med Chem 50: 3777-85 (2007)
Gsk
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.
J Am Chem Soc 129: 9613-5 (2007)
University Of California Berkeley
Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.
J Biol Chem 282: 28709-20 (2007)
Kumamoto University Graduate School Of Medical And Pharmaceutical Sciences
Identification and mechanistic characterization of low-molecular-weight inhibitors for HuR.
Nat Chem Biol 3: 508-15 (2007)
Novartis Institutes For Biomedical Research
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.
Bioorg Med Chem Lett 17: 5245-50 (2007)
Pfizer
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.
Chem Biol Drug Des 70: 1-12 (2007)
Abbott Laboratories
Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPalpha and TPbeta isoforms of the human thromboxane A2 receptor.
J Med Chem 50: 3928-36 (2007)
University Of LièGe
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
J Med Chem 50: 3851-6 (2007)
Novartis Institutes For Biomedical Research
Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.
J Med Chem 50: 3964-8 (2007)
Università
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
Proc Natl Acad Sci U S A 104: 12282-7 (2007)
University Of North Carolina
Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 17: 5165-70 (2007)
Neurocrine Biosciences
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.
Bioorg Med Chem Lett 17: 5218-21 (2007)
Glaxosmithkline
Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.
Bioorg Med Chem Lett 17: 5256-60 (2007)
Ranbaxy Research Laboratories
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
Bioorg Med Chem Lett 17: 5214-7 (2007)
Glaxosmithkline
Discovery and SAR studies of novel GlyT1 inhibitors.
Bioorg Med Chem Lett 17: 5233-8 (2007)
Eli Lilly
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Bioorg Med Chem 15: 6043-53 (2007)
Seoul National University
Inhibition of the bacterial heme oxygenases from Pseudomonas aeruginosa and Neisseria meningitidis: novel antimicrobial targets.
J Med Chem 50: 3804-13 (2007)
University Of Maryland
Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.
J Biol Chem 282: 26316-25 (2007)
University Of Bern
Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
J Med Chem 50: 3765-76 (2007)
National Institute On Drug Abuse
Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists.
Bioorg Med Chem 15: 6208-26 (2007)
Wyeth Research
Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.
Bioorg Med Chem Lett 17: 5239-44 (2007)
Korea Research Institute Of Chemical Technology
Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers.
Bioorg Med Chem Lett 17: 4729-32 (2007)
Chiba University
Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors.
Eur J Med Chem 43: 657-61 (2008)
Università
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.
J Biol Chem 282: 27781-91 (2007)
Pfizer
Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands.
J Biol Chem 282: 26284-93 (2007)
Niddk
Synthesis and antiviral evaluation of 6-(alkyl-heteroaryl)furo[2,3-d]pyrimidin-2(3H)-one nucleosides and analogues with ethynyl, ethenyl, and ethyl spacers at C6 of the furopyrimidine core.
J Med Chem 50: 3897-905 (2007)
Brigham Young University
Novel antagonists of the thioesterase domain of human fatty acid synthase.
Mol Cancer Ther 6: 2120-6 (2007)
Burnham Institute For Medical Research
In vitro suppression of K65R reverse transcriptase-mediated tenofovir- and adefovir-5'-diphosphate resistance conferred by the boranophosphonate derivatives.
Antimicrob Agents Chemother 51: 3162-7 (2007)
Afmb-Cnrs-Esil
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
Antimicrob Agents Chemother 51: 3147-54 (2007)
Glaxosmithkline
Design and synthesis of a library of tertiary amides: evaluation as mimetics of the melanocortins' active core.
Bioorg Med Chem 15: 5787-810 (2007)
Uppsala University
Synthesis, biological evaluation, and molecular modeling of 3,5-substituted-N1-phenyl-N4,N4-di-n-butylsulfanilamides as antikinetoplastid antimicrotubule agents.
Bioorg Med Chem 15: 6071-9 (2007)
The Ohio State University
Mycophenolic acid as a latent agonist of PPARgamma.
Bioorg Med Chem Lett 17: 4767-70 (2007)
Hokkaido University
Pyridinylimidazole inhibitors of Tie2 kinase.
Bioorg Med Chem Lett 17: 4756-60 (2007)
Glaxosmithkline
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.
Bioorg Med Chem Lett 17: 4812-8 (2007)
Mahidol University
Bioactive peroxides as potential therapeutic agents.
Eur J Med Chem 43: 223-51 (2008)
The Hebrew University Of Jerusalem
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.
Mol Pharmacol 72: 876-84 (2007)
Nih
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.
J Biol Chem 282: 27126-32 (2007)
University Of WÜRzburg
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
Bioorg Med Chem Lett 17: 4799-803 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Bioorg Med Chem Lett 17: 4737-45 (2007)
Glaxosmithkline
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.
Bioorg Med Chem Lett 17: 4795-8 (2007)
Merck Research Laboratories
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
J Med Chem 50: 3825-40 (2007)
University Of California Davis
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists.
J Med Chem 50: 3786-94 (2007)
Jerini
Hydroxyethylene isosteres of selective neuronal nitric oxide synthase inhibitors.
Bioorg Med Chem 15: 6096-108 (2007)
Northwestern University
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
Bioorg Med Chem Lett 17: 4824-8 (2007)
Eli Lilly
A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics.
Bioorg Med Chem 15: 5775-86 (2007)
Hacettepe University
4-Amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes as potent FLT-3 inhibitors.
Bioorg Med Chem Lett 17: 4861-5 (2007)
Johnson And Johnson Pharmaceutical Research And Development
Prenylated xanthones from the root bark of Cudrania tricuspidata.
J Nat Prod 70: 1207-9 (2007)
Chungbuk National University
Rationally designed dual inhibitors of HIV reverse transcriptase and integrase.
J Med Chem 50: 3416-9 (2007)
TBA
Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta.
J Med Chem 50: 3954-63 (2007)
Johnson & Johnson Pharmaceutical
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
J Med Chem 50: 3427-30 (2007)
TBA
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
Proc Natl Acad Sci U S A 104: 11927-32 (2007)
The Scripps Research Institute
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Bioorg Med Chem 15: 6170-81 (2007)
Wyeth Research
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bioorg Med Chem Lett 17: 4947-54 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 4432-6 (2007)
Bristol-Myers Squibb Research And Development
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.
Bioorg Med Chem Lett 17: 4746-52 (2007)
Altana Pharma
2D Quantitative structure-activity relationship studies on a series of cholesteryl ester transfer protein inhibitors.
Bioorg Med Chem 15: 6242-52 (2007)
Universidade Federal Da Bahia
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.
Bioorg Med Chem 15: 6109-18 (2007)
University Of Vienna
alpha,alpha-Cyclic aminoacids as useful scaffolds for the preparation of hNK(2) receptor antagonists.
Bioorg Med Chem Lett 17: 4841-4 (2007)
Menarini Ricerche
Synthesis and pharmacochemical evaluation of novel aryl-acetic acid inhibitors of lipoxygenase, antioxidants, and anti-inflammatory agents.
Bioorg Med Chem 15: 5819-27 (2007)
Aristotle University Of Thessaloniki
Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs.
Bioorg Med Chem Lett 17: 4878-81 (2007)
Università
Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists.
Bioorg Med Chem Lett 17: 4845-50 (2007)
Schering-Plough Research Institute
Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.
Bioorg Med Chem Lett 17: 4855-60 (2007)
Virginia Commonwealth University
QSAR study of heparanase inhibitors activity using artificial neural networks and Levenberg-Marquardt algorithm.
Eur J Med Chem 43: 548-56 (2008)
Sharif University Of Technology
3D-QSAR and docking studies of aminopyridine carboxamide inhibitors of c-Jun N-terminal kinase-1.
Eur J Med Chem 43: 604-13 (2008)
Chinese Academy Of Sciences
Synthesis and adenosine receptor binding studies of some novel triazolothienopyrimidines.
Eur J Med Chem 43: 614-20 (2008)
University College Of Pharmaceutical Sciences
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
J Med Chem 50: 3686-95 (2007)
Research Triangle Institute
Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists.
J Med Chem 50: 3585-95 (2007)
University Paris Descartes
Rational optimization of the binding affinity of CD4 targeting peptidomimetics with potential anti HIV activity.
J Med Chem 50: 3482-8 (2007)
University Of Hamburg
Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.
J Med Chem 50: 3561-72 (2007)
Radiopharmaceuticals Research Institute
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.
Bioorg Med Chem 15: 5837-44 (2007)
Astellas Pharma
Functionalization of the 6,14-bridge of the orvinols. Part 3: preparation and pharmacological evaluation of 18- and 19-hydroxyl substituted orvinols.
Bioorg Med Chem Lett 17: 4829-31 (2007)
University Of Maryland
Indanylacetic acids as PPAR-delta activator insulin sensitizers.
Bioorg Med Chem Lett 17: 4369-73 (2007)
Bayer Research Center
Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Bioorg Med Chem Lett 17: 4837-40 (2007)
Biovitrum
Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK.
Bioorg Med Chem Lett 17: 4982-6 (2007)
Meiji Seika Kaisha
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
Bioorg Med Chem Lett 17: 4363-8 (2007)
Gsk
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.
J Biol Chem 282: 27354-65 (2007)
University Of Copenhagen
Design, synthesis, and discovery of stilbene derivatives based on lithospermic acid B as potent protein tyrosine phosphatase 1B inhibitors.
Bioorg Med Chem Lett 17: 4481-6 (2007)
Yonsei University
Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the insulin mimic demethylasterriquinone B1.
J Med Chem 50: 3423-6 (2007)
TBA
Interactions of ceftobiprole with beta-lactamases from molecular classes A to D.
Antimicrob Agents Chemother 51: 3089-95 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta.
J Med Chem 50: 3465-81 (2007)
National Cancer Institute-Frederick
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.
J Med Chem 50: 3442-56 (2007)
Pfizer
Modification of eukaryotic initiation factor 5A from Plasmodium vivax by a truncated deoxyhypusine synthase from Plasmodium falciparum: An enzyme with dual enzymatic properties.
Bioorg Med Chem 15: 6200-7 (2007)
Institute For Medical Parasitology
Structure-based design of alpha-amido aldehyde containing gluten peptide analogues as modulators of HLA-DQ2 and transglutaminase 2.
Bioorg Med Chem 15: 6253-61 (2007)
Stanford University
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Bioorg Med Chem Lett 17: 4415-8 (2007)
Pfizer
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
Bioorg Med Chem Lett 17: 4929-33 (2007)
Merck Frosst Centre For Therapeutic Research
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.
Science 316: 1759-1761 (2007)
Anacor Pharmaceuticals
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease.
Science 317: 516-9 (2007)
Harvard Medical School
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.
Bioorg Med Chem Lett 17: 4873-7 (2007)
Universidad De Santiago De Compostela
Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk.
Bioorg Med Chem Lett 17: 4961-6 (2007)
Institute Of Research
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
Bioorg Med Chem Lett 17: 4630-4 (2007)
Merck Research Laboratories
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
Bioorg Med Chem Lett 17: 4419-27 (2007)
Bristol-Myers Squibb
Agonist lead identification for the high affinity niacin receptor GPR109a.
Bioorg Med Chem Lett 17: 4914-9 (2007)
Arena Pharmaceuticals
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett 17: 4895-900 (2007)
The University Of Tokyo
New chemical tools for investigating human mitotic kinesin Eg5.
Bioorg Med Chem 15: 6474-88 (2007)
Cnrs-Université
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.
Bioorg Med Chem Lett 17: 4901-5 (2007)
Argenta Discovery
Gypsophin: a novel alpha-glucosidase inhibitory cyclic peptide from the roots of Gypsophila oldhamiana.
Bioorg Med Chem Lett 17: 4460-3 (2007)
China Pharmaceutical University
Interaction of O-(undec-10-en)-yl-D-glucose derivatives with the Plasmodium falciparum hexose transporter (PfHT).
Bioorg Med Chem Lett 17: 4934-7 (2007)
Université
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
Bioorg Med Chem Lett 17: 4442-6 (2007)
Tanabe Research Laboratories Usa
Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma.
Bioorg Med Chem Lett 17: 4382-6 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors.
J Med Chem 50: 3751-5 (2007)
Washington University
From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor.
J Med Chem 50: 3706-15 (2007)
Università
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).
J Med Chem 50: 3730-42 (2007)
Bristol-Myers Squibb
Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.
J Med Chem 50: 3420-2 (2007)
TBA
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
J Med Chem 50: 3528-39 (2007)
Amgen
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
J Med Chem 50: 3515-27 (2007)
Amgen
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
J Med Chem 50: 3497-514 (2007)
Amgen
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.
J Med Chem 50: 3627-44 (2007)
Abbott Laboratories
Synthesis of unnatural flavonoids and stilbenes by exploiting the plant biosynthetic pathway in Escherichia coli.
Chem Biol 14: 613-21 (2007)
University Of Tokyo
Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum.
J Nat Prod 70: 1118-21 (2007)
Griffith University
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.
J Nat Prod 70: 1093-7 (2007)
Korean Research Institute Of Biosciences And Biotechnology
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.
Bioorg Med Chem Lett 17: 4374-7 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Bioorg Med Chem Lett 17: 4437-41 (2007)
Boehringer Ingelheim (Canada)
Aminopyrrolidineamide inhibitors of site-1 protease.
Bioorg Med Chem Lett 17: 4411-4 (2007)
Pfizer
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
J Med Chem 50: 3651-60 (2007)
Abbott Laboratories
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.
J Med Chem 50: 3431-3 (2007)
TBA
Platinum complexes can inhibit matrix metalloproteinase activity: platinum-diethyl[(methylsulfinyl)methyl]phosphonate complexes as inhibitors of matrix metalloproteinases 2, 3, 9, and 12.
J Med Chem 50: 3434-41 (2007)
Università
Synthesis and biological activities of isogranulatimide analogues.
Bioorg Med Chem 15: 5965-80 (2007)
Université
Design, synthesis, and molecular modeling studies of 5'-deoxy-5'-ureidoadenosine: 5'-ureido group as multiple hydrogen bonding donor in the active site of S-adenosylhomocysteine hydrolase.
Bioorg Med Chem Lett 17: 4456-9 (2007)
Ewha Womans University
Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors.
Eur J Med Chem 43: 315-26 (2008)
University Of Antwerp
Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor.
Eur J Med Chem 43: 513-39 (2008)
Monash University (Parkville Campus)
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.
Chem Biol Drug Des 69: 444-50 (2007)
Pfizer
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
J Med Chem 50: 3596-603 (2007)
The University Of Iowa
Dual aromatase-steroid sulfatase inhibitors.
J Med Chem 50: 3540-60 (2007)
University Of Bath
Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase.
J Med Chem 50: 3661-6 (2007)
Institute For Natural Products Research And Infection Biology
Multistructure 3D-QSAR studies on a series of conformationally constrained butyrophenones docked into a new homology model of the 5-HT2A receptor.
J Med Chem 50: 3242-55 (2007)
Universitat Pompeu Fabra
Synthesis and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems.
J Med Chem 50: 3314-21 (2007)
Purdue University
SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.
J Med Chem 50: 3222-8 (2007)
Kyoto University
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.
J Med Chem 50: 3194-204 (2007)
Washington University
Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand.
Bioorg Med Chem 15: 5811-8 (2007)
Cairo University
Benzo[b]thiophene-based histone deacetylase inhibitors.
Bioorg Med Chem Lett 17: 4562-7 (2007)
Merck Research Laboratories
The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.
Bioorg Med Chem Lett 17: 4664-9 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.
Bioorg Med Chem Lett 17: 4678-82 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and matrix metalloproteinase (MMP)-12 inhibitory activity of ageladine A and its analogs.
Bioorg Med Chem Lett 17: 4495-9 (2007)
Kyorin Pharmaceutical
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.
Bioorg Med Chem Lett 17: 4509-13 (2007)
Schering-Plough Research Institute
Inhibitors of anthrax lethal factor.
Bioorg Med Chem Lett 17: 4575-8 (2007)
Purdue University
Aza analogues of equol: novel ligands for estrogen receptor beta.
Bioorg Med Chem 15: 5828-36 (2007)
Chinese Academy Of Sciences
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Bioorg Med Chem 15: 5912-49 (2007)
Pfizer
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 17: 4464-70 (2007)
Institut Henri Beaufour
SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.
Bioorg Med Chem Lett 17: 4378-81 (2007)
Bayer Research Center
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.
Bioorg Med Chem Lett 17: 4557-61 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARgamma activators.
Bioorg Med Chem Lett 17: 4613-8 (2007)
National Institute Of Pharmaceutical Education And Research
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
Bioorg Med Chem Lett 17: 4487-90 (2007)
Bristol-Myers Squibb Research And Development
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.
Bioorg Med Chem Lett 17: 4538-44 (2007)
Pfizer
Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.
Bioorg Med Chem Lett 17: 4531-7 (2007)
Pfizer
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.
Bioorg Med Chem Lett 17: 4450-5 (2007)
Glaxosmithkline
Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.
Eur J Med Chem 43: 166-73 (2008)
Sun Yat-Sen University
Enzymatic therapeutic index of acyclovir. Viral versus human polymerase gamma specificity.
J Biol Chem 282: 25159-67 (2007)
The University Of Texas
Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.
J Biol Chem 282: 24504-13 (2007)
Emmy Noether Research Group
SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: taming hERG.
Bioorg Med Chem 15: 5369-85 (2007)
Schering-Plough Research Institute
Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.
Bioorg Med Chem Lett 17: 4248-53 (2007)
Mcgill University/Royal Victoria Hospital
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
J Med Chem 50: 3256-66 (2007)
National Institute Of Mental Health
Enaminone amides as novel orally active GABAA receptor modulators.
J Med Chem 50: 3369-79 (2007)
University Of California Irvine
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Bioorg Med Chem Lett 17: 4657-63 (2007)
Pfizer
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Bioorg Med Chem Lett 17: 3880-5 (2007)
Vernalis (R&D)
A novel arginine methyltransferase inhibitor with cellular activity.
Bioorg Med Chem Lett 17: 4150-3 (2007)
Albert-Ludwigs-University Of Freiburg
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.
J Med Chem 50: 3283-9 (2007)
Southern Research Institute
Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
J Med Chem 50: 3388-91 (2007)
Research Triangle Institute
RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.
Nature 447: 864-868 (2007)
Columbia University
Exploitation of structural and regulatory diversity in glutamate racemases.
Nature 447: 817-822 (2007)
Astrazeneca Global Structural Chemistry
X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy.
J Biol Chem 282: 25436-44 (2007)
Jacobus Pharmaceutical
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.
J Med Chem 50: 3267-73 (2007)
Nci-Fcrdc
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.
Bioorg Med Chem Lett 17: 4568-74 (2007)
Pfizer
Synthesis of symmetrical C- and pseudo-symmetrical O-linked disaccharide analogs for arabinosyltransferase inhibitory activity in Mycobacterium tuberculosis.
Bioorg Med Chem Lett 17: 4527-30 (2007)
Southern Research Institute
Reversine increases the plasticity of lineage-committed mammalian cells.
Proc Natl Acad Sci U S A 104: 10482-7 (2007)
The Scripps Research Institute
P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring.
J Med Chem 50: 3229-41 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
2-tert-butyl-8-quinolinamines exhibit potent blood schizontocidal antimalarial activity via inhibition of heme crystallization.
Antimicrob Agents Chemother 51: 2842-7 (2007)
Kyoto Institute Of Technology
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.
J Biol Chem 282: 24463-70 (2007)
Stony Brook University
Synthesis and biological evaluation of cyclic and branched peptide analogues as ligands for cholecystokinin type 1 receptor.
Bioorg Med Chem 15: 5845-53 (2007)
Istituto Di Biostrutture E Bioimmagini-Cnr
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.
Bioorg Med Chem 15: 5519-28 (2007)
Gilead Sciences
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 17: 4579-83 (2007)
Merck Research Laboratories
N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.
Bioorg Med Chem Lett 17: 4599-603 (2007)
Pfizer
A chemometric study of the 5-HT(1A) receptor affinities presented by arylpiperazine compounds.
Eur J Med Chem 43: 364-72 (2008)
Universidade De S£O Paulo
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.
Bioorg Med Chem 15: 5406-16 (2007)
Universit£
Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists.
Bioorg Med Chem 15: 5590-603 (2007)
Neurocrine Biosciences
Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.
Bioorg Med Chem 15: 5576-89 (2007)
Pfizer
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.
Bioorg Med Chem Lett 17: 4670-7 (2007)
Glaxosmithkline
Design of a partial PPARdelta agonist.
Bioorg Med Chem Lett 17: 4625-9 (2007)
Novo Nordisk
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands.
Bioorg Med Chem 15: 5440-7 (2007)
Santaris Pharma
Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SK(Ca)).
Bioorg Med Chem 15: 5457-79 (2007)
University College London
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Bioorg Med Chem Lett 17: 4242-7 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis of 4-phenoxybenzamide adenine dinucleotide as NAD analogue with inhibitory activity against enoyl-ACP reductase (InhA) of Mycobacterium tuberculosis.
Bioorg Med Chem Lett 17: 4588-91 (2007)
University Of Minnesota
Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators.
Bioorg Med Chem Lett 17: 4118-22 (2007)
University Of Illinois
Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.
Bioorg Med Chem Lett 17: 4646-9 (2007)
Pharmacia
New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold.
J Med Chem 50: 3397-401 (2007)
Vrije Universiteit Brussel
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
J Med Chem 50: 3359-68 (2007)
The Scripps Research Institute
NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor.
Proteins 69: 97-111 (2007)
India Central Drug Research Institute
Phenotypic and structural analyses of hepatitis C virus NS3 protease Arg155 variants: sensitivity to telaprevir (VX-950) and interferon alpha.
J Biol Chem 282: 22619-28 (2007)
Vertex Pharmaceuticals
Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism.
J Biol Chem 282: 23231-9 (2007)
Novartis
Design of novel histone deacetylase inhibitors.
Bioorg Med Chem Lett 17: 4619-24 (2007)
Merck Research Laboratories
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.
Bioorg Med Chem Lett 17: 4683-8 (2007)
Daiichi Pharmaceutical
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.
J Med Chem 50: 3159-62 (2007)
Ewha Womans University
Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors.
J Med Chem 50: 3274-82 (2007)
Purdue University
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.
J Med Chem 50: 3392-6 (2007)
University Of Minnesota
Structural variation governs substrate specificity for organic anion transporter (OAT) homologs. Potential remote sensing by OAT family members.
J Biol Chem 282: 23841-53 (2007)
University Of California
3D-QSAR studies on sildenafil analogues, selective phosphodiesterase 5 inhibitors.
Bioorg Med Chem Lett 17: 4271-4 (2007)
Sungkyunkwan University
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
Bioorg Med Chem Lett 17: 4144-9 (2007)
Re&D Vufb
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
Bioorg Med Chem Lett 17: 4158-62 (2007)
Ligand Pharmaceuticals
Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
Bioorg Med Chem Lett 17: 4689-93 (2007)
Kowa
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
J Med Chem 50: 3163-6 (2007)
University Of Michigan
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.
J Med Chem 50: 3015-3025 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates.
J Med Chem 50: 3046-3053 (2007)
Duquesne University
Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
J Med Chem 50: 3143-7 (2007)
Ewha Womans University
Bidirectional, iterative approach to the structural delineation of the functional"chemoprint" in GPR40 for agonist recognition.
J Med Chem 50: 2981-9 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action.
Bioorg Med Chem 15: 5563-75 (2007)
Dipartimento Di Scienze Farmaceutiche
Extension of Drosophila melanogaster life span with a GPCR peptide inhibitor.
Nat Chem Biol 3: 415-9 (2007)
California Institute Of Technology
Activation of inhibitors by sortase triggers irreversible modification of the active site.
J Biol Chem 282: 23129-39 (2007)
University Of Chicago
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.
Bioorg Med Chem Lett 17: 4167-72 (2007)
Lg Life Sciences
Synthesis and biological evaluation of 9-deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid as multi-substrate analogue inhibitors of PNP.
Bioorg Med Chem Lett 17: 4173-7 (2007)
Tokyo University Of Pharmacy And Life Sciences
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Bioorg Med Chem 15: 5166-76 (2007)
Neurocrine Biosciences
Synthesis, 3D-QSAR, and docking studies of 1-phenyl-1H-1,2,3-triazoles as selective antagonists for beta3 over alpha1beta2gamma2 GABA receptors.
Bioorg Med Chem 15: 5090-104 (2007)
Shimane University
Targeting cytochrome P450 enzymes: a new approach in anti-cancer drug development.
Bioorg Med Chem 15: 5047-60 (2007)
University Of Maryland
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
Bioorg Med Chem Lett 17: 3819-25 (2007)
Berlex Biosciences
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.
Bioorg Med Chem Lett 17: 4308-15 (2007)
Abbott Laboratories
Primary amides as selective inhibitors of cathepsin K.
Bioorg Med Chem Lett 17: 4328-32 (2007)
Merck Frosst Centre For Therapeutic Research
5-Arylidene-2,4-thiazolidinediones as inhibitors of protein tyrosine phosphatases.
Bioorg Med Chem 15: 5137-49 (2007)
Universit£
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.
Bioorg Med Chem Lett 17: 4131-4 (2007)
Karo Bio
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.
Bioorg Med Chem Lett 17: 4128-30 (2007)
Harvard Medical School
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
Bioorg Med Chem Lett 17: 4284-9 (2007)
Bristol-Myers Squibb
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
Bioorg Med Chem Lett 17: 4191-5 (2007)
Polaris Pharmaceuticals
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.
Chem Biol Drug Des 69: 331-7 (2007)
Chemdiv
Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.
Chem Biol Drug Des 69: 298-313 (2007)
University Of Maryland
Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies.
J Med Chem 50: 3054-61 (2007)
University Of Illinois At Chicago
Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.
J Med Chem 50: 3138-3142 (2007)
Universita Degli Studi
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.
J Med Chem 50: 3062-9 (2007)
Institut D'Investigacions BiomèDiques August Pi I
Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis.
Proc Natl Acad Sci U S A 104: 10619-24 (2007)
Pfizer
Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
J Biol Chem 282: 20847-53 (2007)
Institute For Medical Research
Isolation of glycosidase-inhibiting hyacinthacines and related alkaloids from Scilla socialis.
J Nat Prod 70: 993-7 (2007)
University Of Toyama
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
J Med Chem 50: 3101-12 (2007)
James Black Foundation
Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors
J Med Chem 50: 2967-80 (2007)
Berlex Biosciences
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
J Med Chem 50: 2931-41 (2007)
Pfizer
Small-molecule activators of RNase L with broad-spectrum antiviral activity.
Proc Natl Acad Sci U S A 104: 9585-90 (2007)
Lerner Research Institute
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
Proc Natl Acad Sci U S A 104: 10022-7 (2007)
Institute Of Biological Chemistry
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
J Biol Chem 282: 20836-46 (2007)
Merck Research Laboratories
Potent macrocyclic antagonists to the motilin receptor presenting novel unnatural amino acids.
Bioorg Med Chem Lett 17: 4187-90 (2007)
Tranzyme Pharma
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Bioorg Med Chem Lett 17: 4290-6 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Bioorg Med Chem Lett 17: 3916-20 (2007)
Glaxosmithkline
Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists.
Bioorg Med Chem 15: 5177-90 (2007)
University Of Tokyo
Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists.
Bioorg Med Chem Lett 17: 4228-31 (2007)
Ucb Pharma
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Bioorg Med Chem Lett 17: 4297-302 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors.
Bioorg Med Chem Lett 17: 4208-12 (2007)
Nagoya City University
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.
Eur J Med Chem 43: 456-63 (2008)
University Of Alexandria
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Bioorg Med Chem Lett 17: 4303-7 (2007)
Abbott Laboratories
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists.
Bioorg Med Chem Lett 17: 4232-41 (2007)
Astrazeneca R&D MöLndal
C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase.
Bioorg Med Chem Lett 17: 3835-9 (2007)
Roche Research Center
Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: evaluation of in vitro anti-cancer and anti-folate activities.
Eur J Med Chem 43: 189-203 (2008)
Università
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.
Bioorg Med Chem Lett 17: 4323-7 (2007)
Emd-Serono Research Institute
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
Bioorg Med Chem Lett 17: 3814-8 (2007)
Berlex Biosciences
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.
Bioorg Med Chem Lett 17: 4333-7 (2007)
Wyeth Research
Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents.
Bioorg Med Chem Lett 17: 4338-42 (2007)
Yale University
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Bioorg Med Chem Lett 17: 4347-50 (2007)
Novartis Institutes Of Biomedical Research
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.
Bioorg Med Chem Lett 17: 3925-9 (2007)
Shionogi
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.
J Med Chem 50: 3086-100 (2007)
Abbott Laboratories
Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria.
Antimicrob Agents Chemother 51: 2726-32 (2007)
University Of Copenhagen
Alternative chemical modifications reverse the binding orientation of a pharmacophore scaffold in the active site of macrophage migration inhibitory factor.
J Biol Chem 282: 23089-95 (2007)
Yale University
Alkyl-CoA disulfides as inhibitors and mechanistic probes for FabH enzymes.
Chem Biol 14: 513-24 (2007)
Portland State University
Structure-activity relationships of semisynthetic mumbaistatin analogs.
Bioorg Med Chem 15: 5207-18 (2007)
Stanford University
QSAR study of selective ligands for the thyroid hormone receptor beta.
Bioorg Med Chem 15: 5251-61 (2007)
University Of Insubria
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.
Bioorg Med Chem Lett 17: 4351-7 (2007)
Nagoya City University
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Bioorg Med Chem Lett 17: 3864-7 (2007)
Glaxosmithkline
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
Bioorg Med Chem Lett 17: 3921-4 (2007)
University Of Shizuoka
Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.
Bioorg Med Chem Lett 17: 3855-9 (2007)
Johnson And Johnson Pharmaceutical Research And Development
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.
J Med Chem 50: 2990-3003 (2007)
Abbott Laboratories
The biology and chemistry of hyperlipidemia.
Bioorg Med Chem 15: 4674-99 (2007)
Sinhgad College Of Pharmacy
Human and rat monoamine oxidase-A are differentially inhibited by (S)-4-alkylthioamphetamine derivatives: insights from molecular modeling studies.
Bioorg Med Chem 15: 5198-206 (2007)
University Of Santiago De Chile
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.
Bioorg Med Chem Lett 17: 3845-50 (2007)
Neurocrine Biosciences
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.
Bioorg Med Chem Lett 17: 4030-4 (2007)
Shionogi
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.
J Med Chem 50: 2875-85 (2007)
The National Hellenic Research Foundation
The inhibitory effect of some new synthesized xanthates on mushroom tyrosinase activities.
J Enzyme Inhib Med Chem 22: 239-46 (2007)
University Of Tehran
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
Antimicrob Agents Chemother 51: 2911-9 (2007)
Mcgill University
7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands.
Bioorg Med Chem 15: 5239-50 (2007)
Jagiellonian University Medical College
Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system.
Bioorg Med Chem 15: 4876-90 (2007)
Universitat De Barcelona
QSAR studies and pharmacophore identification for arylsubstituted cycloalkenecarboxylic acid methyl esters with affinity for the human dopamine transporter.
Bioorg Med Chem 15: 5262-74 (2007)
University Of Aarhus
Synthesis and evaluation of homo-bivalent GnRHR ligands.
Bioorg Med Chem 15: 4841-56 (2007)
Leiden University
Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.
Bioorg Med Chem 15: 5316-21 (2007)
Università
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Bioorg Med Chem Lett 17: 3930-4 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.
Bioorg Med Chem Lett 17: 3769-73 (2007)
Zhengzhou University
Inhibitory effect of 2-arylbenzofurans from Erythrina addisoniae on protein tyrosine phosphatase-1B.
Bioorg Med Chem Lett 17: 3868-71 (2007)
Korea Research Institute Of Bioscience And Biotechnology
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
J Med Chem 50: 2779-86 (2007)
University Of Arizona Tucson
Crystal structures of Saccharomyces cerevisiae N-myristoyltransferase with bound myristoyl-CoA and inhibitors reveal the functional roles of the N-terminal region.
J Biol Chem 282: 22185-94 (2007)
Chinese Academy Of Sciences
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.
Bioorg Med Chem Lett 17: 3939-42 (2007)
University Of Michigan
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Bioorg Med Chem Lett 17: 3978-82 (2007)
Pharmaceutical Research Institute
Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I.
Bioorg Med Chem Lett 17: 3793-7 (2007)
University Of Minnesota
Quantitative structure activity relationship studies on thiourea analogues as influenza virus neuraminidase inhibitors.
Eur J Med Chem 43: 293-9 (2008)
National Institute Of Pharmaceutical Education And Research (Niper)
Structure-based discovery of a new class of Bcl-xL antagonists.
Bioorg Chem 35: 344-53 (2007)
Burnham Institute For Medical Research
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies.
Bioorg Med Chem 15: 4753-66 (2007)
Université
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-opioid agonists with potential anxiolytic/antidepressant properties. Part 2.
Bioorg Med Chem Lett 17: 3860-3 (2007)
Johnson & Johnson Pharmaceutical Research & Development
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
Bioorg Med Chem Lett 17: 3988-91 (2007)
Novartis Institutes For Biomedical Research
Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.
Bioorg Med Chem Lett 17: 3630-5 (2007)
Pfizer
Evaluation of in vitro aldose redutase inhibitory activity of 5-arylidene-2,4-thiazolidinediones.
Bioorg Med Chem Lett 17: 3886-93 (2007)
Universit£
Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
J Med Chem 50: 2799-806 (2007)
Purdue University
O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies.
Bioorg Med Chem 15: 4767-74 (2007)
National Cancer Institute At Frederick
New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.
Bioorg Med Chem Lett 17: 3943-6 (2007)
Université
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
Bioorg Med Chem Lett 17: 3595-8 (2007)
Seoul National University
Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.
Bioorg Med Chem Lett 17: 3652-6 (2007)
Adolor
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.
Bioorg Med Chem Lett 17: 3983-7 (2007)
Novartis Institutes For Biomedical Research
Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.
Bioorg Med Chem Lett 17: 3969-71 (2007)
Merck Research Laboratories
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Bioorg Med Chem Lett 17: 3894-9 (2007)
Abbott Laboratories
Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor.
J Med Chem 50: 2903-15 (2007)
Medical University Of Lublin
Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.
J Med Chem 50: 2818-41 (2007)
Cardiome Pharma
Fawcettimine-related alkaloids from Lycopodium serratum.
J Nat Prod 70: 1024-8 (2007)
Chiba University
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrob Agents Chemother 51: 2445-53 (2007)
Achillion Pharmaceuticals
Pyrophosphorolytic excision of nonobligate chain terminators by hepatitis C virus NS5B polymerase.
Antimicrob Agents Chemother 51: 2920-8 (2007)
Mcgill University
Discovery of structurally diverse HIV-1 integrase inhibitors based on a chalcone pharmacophore.
Bioorg Med Chem 15: 4985-5002 (2007)
University Of Southern California
Inhibition of IGF-1R and lipoxygenase by nordihydroguaiaretic acid (NDGA) analogs.
Bioorg Med Chem Lett 17: 4026-9 (2007)
San Francisco State University
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.
Bioorg Med Chem Lett 17: 3972-7 (2007)
Gsk
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 3910-5 (2007)
Bristol-Myers Squibb
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.
Bioorg Med Chem Lett 17: 3877-9 (2007)
Merck Research Laboratories
Radioiodinated aza-diphenylacetylenes as potential SPECT imaging agents for beta-amyloid plaque detection.
Bioorg Med Chem Lett 17: 3581-4 (2007)
University Of Pennsylvania
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Bioorg Med Chem Lett 17: 4006-11 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
Bioorg Med Chem Lett 17: 3511-5 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis, in vitro antiproliferative activities, and Chk1 inhibitory properties of pyrrolo[3,4-a]carbazole-1,3-diones, pyrrolo[3,4-c]carbazole-1,3-diones, and 2-aminopyridazino[3,4-a]pyrrolo[3,4-c]carbazole-1,3,4,7-tetraone.
Eur J Med Chem 43: 282-92 (2008)
Université
Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists.
J Med Chem 50: 2807-17 (2007)
Johnson & Johnson Pharmaceutical
Synthesis and in vitro antiplatelet activity of new 4-(1-piperazinyl)coumarin derivatives. Human platelet phosphodiesterase 3 inhibitory properties of the two most effective compounds described and molecular modeling study on their interactions with phosphodiesterase 3A catalytic site.
J Med Chem 50: 2886-95 (2007)
Universit£
Novel heterocyclic thyromimetics. Part 2.
Bioorg Med Chem Lett 17: 3992-6 (2007)
Bayer Healthcare
N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors.
Bioorg Med Chem 15: 5003-17 (2007)
Jagiellonian University
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.
Bioorg Med Chem Lett 17: 4035-9 (2007)
Forschungszentrum Dresden-Rossendorf
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.
Bioorg Med Chem Lett 17: 3660-5 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones.
Bioorg Med Chem Lett 17: 3962-8 (2007)
Università
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.
Bioorg Med Chem Lett 17: 3562-9 (2007)
Kalypsys
A new class of histamine H3 receptor antagonists derived from ligand based design.
Bioorg Med Chem Lett 17: 3670-5 (2007)
F. Hoffmann-La Roche
The discovery of long acting beta2-adrenoreceptor agonists.
Bioorg Med Chem Lett 17: 4012-5 (2007)
Pfizer
Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists.
Bioorg Med Chem Lett 17: 3624-9 (2007)
Pfizer
Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors.
Bioorg Med Chem Lett 17: 3957-61 (2007)
University Of Tokyo
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.
Bioorg Med Chem Lett 17: 3997-4000 (2007)
Merck Research Laboratories
Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1.
J Med Chem 50: 2787-98 (2007)
University Of California San Francisco
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
J Med Chem 50: 2753-66 (2007)
Kobe Gakuin University
Self-assembling cannabinomimetics: supramolecular structures of N-alkyl amides.
J Nat Prod 70: 1010-5 (2007)
Department Of Chemistry And Applied Biosciences
Diarylquinolines target subunit c of mycobacterial ATP synthase.
Nat Chem Biol 3: 323-4 (2007)
Tibotec
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
J Biol Chem 282: 19716-27 (2007)
University Of California
Structures of Mycobacterium tuberculosis 1-deoxy-D-xylulose-5-phosphate reductoisomerase provide new insights into catalysis.
J Biol Chem 282: 19905-16 (2007)
Uppsala University
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
Bioorg Med Chem 15: 4434-43 (2007)
University Of Ferrara
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
Bioorg Med Chem 15: 4396-405 (2007)
Wyeth Research
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Bioorg Med Chem Lett 17: 3618-23 (2007)
Abbott Laboratories
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.
Bioorg Med Chem Lett 17: 3647-51 (2007)
Schering-Plough Research Institute
Evaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5alpha-reductase.
Bioorg Med Chem Lett 17: 3603-7 (2007)
University Of Canterbury
Dihydro-[1H]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia.
Bioorg Med Chem Lett 17: 3491-6 (2007)
Johnson And Johnson Pharmaceutical Research And Development
Isoprenylated flavonoids from the stem bark of Erythrina abyssinica.
J Nat Prod 70: 1039-42 (2007)
Korea Research Institute Of Bioscience And Biotechnology
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.
J Med Chem 50: 2682-92 (2007)
University Of Illinois At Chicago
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate.
J Med Chem 50: 2718-31 (2007)
Georgia Institute Of Technology
An adamantyl-substituted retinoid-derived molecule that inhibits cancer cell growth and angiogenesis by inducing apoptosis and binds to small heterodimer partner nuclear receptor: effects of modifying its carboxylate group on apoptosis, proliferation, and protein-tyrosine phosphatase activity.
J Med Chem 50: 2622-39 (2007)
Burnham Institute For Medical Research
Kv7 (KCNQ) channel modulators and neuropathic pain.
J Med Chem 50: 2576-82 (2007)
Neurosearch
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
J Med Chem 50: 2563-8 (2007)
Eli Lilly
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
J Med Chem 50: 2589-96 (2007)
Glaxosmithkline
Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium.
Proc Natl Acad Sci U S A 104: 8316-21 (2007)
Hebrew University Of Jerusalem
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
J Med Chem 50: 2747-51 (2007)
Chinese Academy Of Sciences
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.
J Med Chem 50: 2767-78 (2007)
Biogen Idec
Mass spectrometry-based systems approach for identification of inhibitors of Plasmodium falciparum fatty acid synthase.
Antimicrob Agents Chemother 51: 2552-8 (2007)
Institute Of Science
Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
Antimicrob Agents Chemother 51: 2403-11 (2007)
University Of California
RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia.
Bioorg Med Chem Lett 17: 3497-503 (2007)
Johnson And Johnson Pharmaceutical Research And Development
3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 17: 3504-7 (2007)
Roche Pharmaceuticals
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.
Bioorg Med Chem Lett 17: 3570-4 (2007)
Eli Lilly
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Proc Natl Acad Sci U S A 104: 8520-5 (2007)
Abbott Laboratories
3D-QSAR studies on malonyl coenzyme A decarboxylase inhibitors.
Bioorg Med Chem 15: 4470-81 (2007)
St. John'S University
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Bioorg Med Chem Lett 17: 4044-8 (2007)
Abbott Laboratories
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Bioorg Med Chem Lett 17: 4057-61 (2007)
Merck Research Laboratories
ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands.
Bioorg Med Chem Lett 17: 4053-6 (2007)
Wyeth Research
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.
Eur J Med Chem 43: 73-80 (2008)
Central Drug Research Institute
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Bioorg Med Chem Lett 17: 3575-80 (2007)
Pfizer
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.
Bioorg Med Chem Lett 17: 3544-9 (2007)
Eli Lilly
3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2.
Bioorg Med Chem Lett 17: 3636-41 (2007)
Merck Research Laboratories
Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.
Bioorg Med Chem Lett 17: 3608-12 (2007)
Merck
Brucella suis histidinol dehydrogenase: synthesis and inhibition studies of a series of substituted benzylic ketones derived from histidine.
Bioorg Med Chem 15: 4427-33 (2007)
Ecole Nationale Sup£Rieure De Chimie De Montpellier
Synthesis and biological activity of new melatonin dimeric derivatives.
Bioorg Med Chem 15: 4643-50 (2007)
Università
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.
Bioorg Med Chem Lett 17: 3266-70 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates.
Bioorg Med Chem Lett 17: 3550-7 (2007)
Chemical Diversity
Bioactive compounds from Bauhinia purpurea possessing antimalarial, antimycobacterial, antifungal, anti-inflammatory, and cytotoxic activities.
J Nat Prod 70: 795-801 (2007)
Chiang Mai University
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
J Med Chem 50: 2647-54 (2007)
Pfizer
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors.
J Med Chem 50: 2700-7 (2007)
University Of Liverpool
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.
J Med Chem 50: 2737-41 (2007)
Kribb
Discovery of a rhodanine class of compounds as inhibitors of Plasmodium falciparum enoyl-acyl carrier protein reductase.
J Med Chem 50: 2665-75 (2007)
Institute Of Science
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
J Med Chem 50: 2597-600 (2007)
Glaxosmithkline
Carbonic anhydrases as targets for medicinal chemistry.
Bioorg Med Chem 15: 4336-50 (2007)
Universit£
Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.
Bioorg Med Chem Lett 17: 3558-61 (2007)
Merck Research Laboratories
2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.
Bioorg Med Chem Lett 17: 3696-701 (2007)
Universit£
Plant P5C reductase as a new target for aminomethylenebisphosphonates.
J Agric Food Chem 55: 4340-7 (2007)
University Of Ferrara
Isoform-selective inhibition of the human UDP-glucuronosyltransferase 2B7 by isolongifolol derivatives.
J Med Chem 50: 2655-64 (2007)
University Of Helsinki
Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship.
J Med Chem 50: 2605-8 (2007)
Mcgill University Health Center/Royal Victoria Hospital
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.
Proc Natl Acad Sci U S A 104: 8059-64 (2007)
University Of California
Binding of ceftobiprole and comparators to the penicillin-binding proteins of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.
Antimicrob Agents Chemother 51: 2621-4 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
Antimicrob Agents Chemother 51: 2600-4 (2007)
Kagoshima University
Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.
Bioorg Med Chem 15: 4618-28 (2007)
Imperial College
Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode.
J Med Chem 50: 2693-9 (2007)
University Of California Berkeley
Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
J Med Chem 50: 2732-6 (2007)
Almirall
2D QSAR studies on thyroid hormone receptor ligands.
Bioorg Med Chem 15: 4609-17 (2007)
Universidade De S£O Paulo
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.
Bioorg Med Chem Lett 17: 3354-61 (2007)
Merck Research Laboratories
Discovery of new C3aR ligands. Part 1: arginine derivatives.
Bioorg Med Chem Lett 17: 3258-61 (2007)
Ucb Pharma
Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.
Bioorg Med Chem Lett 17: 3736-40 (2007)
Ajinomoto
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
Bioorg Med Chem Lett 17: 3760-4 (2007)
Schering-Plough Research Institute
Crystal structures of multidrug binding protein TtgR in complex with antibiotics and plant antimicrobials.
J Mol Biol 369: 829-40 (2007)
Imperial College
A fragment-based approach for the discovery of isoform-specific p38alpha inhibitors.
ACS Chem Biol 2: 329-36 (2007)
Burnham Institute For Medical Research
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.
Proc Natl Acad Sci U S A 104: 7391-6 (2007)
University Of Central Florida College Of Medicine
Docking-based 3D-QSAR study for selectivity of DPP4, DPP8, and DPP9 inhibitors.
Bioorg Med Chem Lett 17: 3716-21 (2007)
Korea Research Institute Of Chemical Technology
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.
Bioorg Med Chem Lett 17: 3322-9 (2007)
Curacyte Discovery
Benzopyran sulfonamides as KV1.5 potassium channel blockers.
Bioorg Med Chem Lett 17: 3271-5 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.
J Med Chem 50: 2609-11 (2007)
Merck Research Laboratories
Identification of natural-product-derived inhibitors of 5-lipoxygenase activity by ligand-based virtual screening.
J Med Chem 50: 2640-6 (2007)
Johann Wolfgang Goethe-UniversitäT
Small-molecule synergist of the Wnt/beta-catenin signaling pathway.
Proc Natl Acad Sci U S A 104: 7444-8 (2007)
The Scripps Research Institute
7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.
Bioorg Med Chem 15: 4543-51 (2007)
University College London
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
Bioorg Med Chem Lett 17: 3778-83 (2007)
Schering-Plough Research Institute
Novel inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 17: 3287-91 (2007)
Bristol-Myers Squibb
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Bioorg Med Chem Lett 17: 3463-7 (2007)
Ucb Pharma
Discovery of new C3aR ligands. Part 2: amino-piperidine derivatives.
Bioorg Med Chem Lett 17: 3262-5 (2007)
Ucb Pharma
Classification of estrogen receptor-beta ligands on the basis of their binding affinities using support vector machine and linear discriminant analysis.
Eur J Med Chem 43: 43-52 (2008)
Yantai University
Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.
J Med Chem 50: 2391-8 (2007)
Tufts University School Of Medicine
De Novo Parallel Design, Synthesis and Evaluation of Inhibitors against the Reverse Transcriptase of Human Immunodeficiency Virus Type-1 and Drug-Resi
J Med Chem 50: 2370-84 (2007)
Bar-Ilan University
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
J Med Chem 50: 2408-14 (2007)
University Of Copenhagen
Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone.
J Med Chem 50: 2520-6 (2007)
Merck Research Laboratories
Nicotinic acid receptor agonists differentially activate downstream effectors.
J Biol Chem 282: 18028-36 (2007)
Arena Pharmaceuticals
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).
Bioorg Med Chem Lett 17: 3292-7 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Exploring molecular shape analysis of styrylquinoline derivatives as HIV-1 integrase inhibitors.
Eur J Med Chem 43: 81-92 (2008)
Jadavpur University
Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation.
Eur J Med Chem 43: 62-72 (2008)
Sapienza University Of Rome
Assessing potency of c-Jun N-terminal kinase 3 (JNK3) inhibitors using 2D molecular descriptors and binary QSAR methodology.
Bioorg Med Chem 15: 4256-64 (2007)
Aureus Pharma
Synthesis and glycogen phosphorylase inhibitor activity of 2,3-dihydrobenzo[1,4]dioxin derivatives.
Bioorg Med Chem 15: 4048-56 (2007)
University Of Debrecen
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 17: 3765-8 (2007)
Sun Yat-Sen University
Indolizidine alkaloids with delta-opioid receptor binding affinity from the leaves of Elaeocarpus fuscoides.
J Nat Prod 70: 872-5 (2007)
Griffith University
Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.
J Med Chem 50: 2289-92 (2007)
Astex
Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery.
J Med Chem 50: 2293-2296 (2007)
Astex
Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitors.
Bioorg Med Chem Lett 17: 3729-32 (2007)
Harvard Medical School
Squalene-derived flexible linkers for bioactive peptides.
Bioorg Med Chem Lett 17: 3310-3 (2007)
University Of Arizona
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.
Bioorg Med Chem Lett 17: 3754-9 (2007)
Cerep
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
Bioorg Med Chem Lett 17: 3339-43 (2007)
Amgen
Bridged androstenediol analogs as ER-beta selective SERMs.
Bioorg Med Chem Lett 17: 2944-8 (2007)
Merck Research Laboratories
Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.
Eur J Med Chem 42: 1084-94 (2007)
Zentiva Vufb
1-Aryl-4,6-dihydropyrazolo[4,3-d][1]benzazepin-5(1H)-ones: a new class of antiproliferative agents with selectivity for human leukemia and breast cancer cell lines.
Eur J Med Chem 42: 1317-24 (2007)
Technische UniversitÄT Braunschweig
New diphenylacetylenes as probes for positron emission tomographic imaging of amyloid plaques.
J Med Chem 50: 2415-23 (2007)
University Of Pennsylvania
Small molecule designed to target metal binding site in the alpha2I domain inhibits integrin function.
J Med Chem 50: 2742-6 (2007)
University Of Turku
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
J Med Chem 50: 2497-505 (2007)
Universidade De Vigo
Enhanced substituted resorcinol hydrophobicity augments tyrosinase inhibition potency.
J Med Chem 50: 2676-81 (2007)
Migal - Galilee Technology Center
A high-throughput screen for aggregation-based inhibition in a large compound library.
J Med Chem 50: 2385-90 (2007)
University Of California San Francisco
Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines.
J Med Chem 50: 2341-51 (2007)
Pfizer
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.
Bioorg Med Chem 15: 4159-74 (2007)
University Of Aarhus
Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging.
Bioorg Med Chem Lett 17: 3458-62 (2007)
Katholieke Universiteit Leuven
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists.
Bioorg Med Chem Lett 17: 3367-72 (2007)
Tanabe Research Laboratories
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
Bioorg Med Chem Lett 17: 2987-91 (2007)
National Institute On Drug Abuse
Synthesis and biological evaluation of 2beta,3alpha-(substituted phenyl)nortropanes as potential norepinephrine transporter imaging agents.
Bioorg Med Chem Lett 17: 3044-7 (2007)
Emory University
Structure-guided optimization of small molecules inhibiting human immunodeficiency virus 1 Tat association with the human coactivator p300/CREB binding protein-associated factor.
J Med Chem 50: 2285-8 (2007)
TBA
Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.
J Med Chem 50: 2310-8 (2007)
Schering-Plough Research Institute
Benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulfonamides as inhibitors of carbonic anhydrase.
Bioorg Med Chem Lett 17: 3335-8 (2007)
Institute Of Biotechnology
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Bioorg Med Chem Lett 17: 3421-5 (2007)
Biovitrum
The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.
Chem Biol Drug Des 69: 204-11 (2007)
Shanghai Jiao Tong University
Synthesis of peptidyl ene diones: selective inactivators of the cysteine proteinases.
Chem Biol Drug Des 69: 170-9 (2007)
Queen'S University Of Belfast
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.
J Med Chem 50: 2297-300 (2007)
Takeda Pharmaceutical
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
J Med Chem 50: 2486-96 (2007)
Ligand Pharmaceuticals
Sensitivity of monkey B virus (Cercopithecine herpesvirus 1) to antiviral drugs: role of thymidine kinase in antiviral activities of substrate analogs and acyclonucleosides.
Antimicrob Agents Chemother 51: 2028-34 (2007)
Glsynthesis
Biochemical characterization of PER-2 and genetic environment of blaPER-2.
Antimicrob Agents Chemother 51: 2359-65 (2007)
Universidad De Buenos Aires
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
J Biol Chem 282: 16379-90 (2007)
Vanderbilt Institute For Chemical Biology
Synthesis and evaluation of amino-threoses in D- and L-series: are five membered ring amino-sugars more potent glycosidase inhibitors than the six membered ones?
Bioorg Med Chem 15: 4125-35 (2007)
Universit£
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.
Bioorg Med Chem Lett 17: 3435-9 (2007)
Daiichi Asubio Pharma
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.
Bioorg Med Chem Lett 17: 3378-83 (2007)
Pfizer
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
Bioorg Med Chem Lett 17: 3388-91 (2007)
Abbott Laboratories
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).
Bioorg Med Chem Lett 17: 3373-7 (2007)
Merck Research Laboratories
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.
Bioorg Med Chem Lett 17: 3344-8 (2007)
Eli Lilly
Caffeoylglycolic and caffeoylamino acid derivatives, halfmers of L-chicoric acid, as new HIV-1 integrase inhibitors.
Eur J Med Chem 42: 1309-15 (2007)
Korea Institute Of Science & Technology
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
Bioorg Med Chem Lett 17: 3349-53 (2007)
Pfizer
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).
Bioorg Med Chem 15: 4136-43 (2007)
Technische UniversitäT MüNchen
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.
Bioorg Med Chem 15: 4077-84 (2007)
Astrazeneca
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Bioorg Med Chem 15: 4106-12 (2007)
Harvard Medical School
Novel 3-galloylamido-N'-substituted-2,6-piperidinedione-N-acetamide peptidomimetics as metalloproteinase inhibitors.
Bioorg Med Chem Lett 17: 2935-8 (2007)
Shandong University
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Bioorg Med Chem Lett 17: 3384-7 (2007)
Merck Research Laboratories
Synthesis and biological activity of imidazopyridine anticoccidial agents: part I.
Eur J Med Chem 42: 1334-57 (2007)
Scynexis
Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.
J Med Chem 50: 2399-407 (2007)
Purdue University
Target-based approach to inhibitors of histone arginine methyltransferases.
J Med Chem 50: 2319-25 (2007)
Albert-Ludwigs-University Of Freiburg
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.
Proc Natl Acad Sci U S A 104: 6846-51 (2007)
Pharmaceutical Research Institute
chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model.
J Biol Chem 282: 17837-44 (2007)
The University Of Queensland
Inhibitory effect of obovatal on the migration and invasion of HT1080 cells via the inhibition of MMP-2.
Bioorg Med Chem 15: 4085-90 (2007)
Korea Research Institute Of Bioscience And Biotechnology
Synthesis of andrographolide derivatives: a new family of alpha-glucosidase inhibitors.
Bioorg Med Chem 15: 4247-55 (2007)
Zhengzhou University
Structure-based organic synthesis of unnatural aeruginosin hybrids as potent inhibitors of thrombin.
Bioorg Med Chem Lett 17: 3480-5 (2007)
Université
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Bioorg Med Chem Lett 17: 3023-7 (2007)
Schering-Plough Research Institute
Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.
Bioorg Med Chem Lett 17: 3006-9 (2007)
Merck
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
J Med Chem 50: 2225-39 (2007)
P. Angeletti S.P.A. (Merck Research Laboratories)
Glyoxylate and pyruvate are antagonistic effectors of the Escherichia coli IclR transcriptional regulator.
J Biol Chem 282: 16476-91 (2007)
University Of Toronto
Novel selective neuropeptide Y2 receptor PEGylated peptide agonists reduce food intake and body weight in mice.
J Med Chem 50: 2264-8 (2007)
Bayer Pharmaceuticals
Virtual screening for novel openers of pancreatic K(ATP) channels.
J Med Chem 50: 2117-26 (2007)
University Of Perugia
Structure-based design and synthesis of N(omega)-nitro-L-arginine-containing peptidomimetics as selective inhibitors of neuronal nitric oxide synthase. Displacement of the heme structural water.
J Med Chem 50: 2089-99 (2007)
Northwestern University
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
J Med Chem 50: 2011-29 (2007)
Abbott Laboratories
Serum differentially alters the antifungal properties of echinocandin drugs.
Antimicrob Agents Chemother 51: 2253-6 (2007)
Public Health Research Institute
Molecular modeling study for the binding of zonisamide and topiramate to the human mitochondrial carbonic anhydrase isoform VA.
Bioorg Med Chem 15: 4152-8 (2007)
Istituto Di Biostrutture E Bioimmagini-Cnr
Calculation of binding energy using BLYP/MM for the HIV-1 integrase complexed with the S-1360 and two analogues.
Bioorg Med Chem 15: 3818-24 (2007)
Universidade Federal Do Par£
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Bioorg Med Chem Lett 17: 3028-33 (2007)
Schering-Plough Research Institute
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Bioorg Med Chem Lett 17: 2927-30 (2007)
Glaxosmithkline
Synthesis of bridged piperazines with sigma receptor affinity.
Eur J Med Chem 42: 1247-62 (2007)
Institut F£R Pharmazeutische Und Medizinische Chemie
Design and synthesis of a potent histone deacetylase inhibitor.
J Med Chem 50: 2003-6 (2007)
Virginia Tech
Novel aminoethylbiphenyls as 5-HT7 receptor ligands.
Bioorg Med Chem Lett 17: 3018-22 (2007)
Université
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.
Bioorg Med Chem Lett 17: 3431-4 (2007)
Daiichi Asubio Pharma
Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.
Bioorg Med Chem Lett 17: 2998-3002 (2007)
Alcon Research
QSAR study on a novel series of 8-azaadenine analogues proposed as A1 adenosine receptor antagonists.
Eur J Med Chem 43: 114-21 (2008)
University Of Pisa
Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 3010-3 (2007)
Pharmacopeia Drug Discovery
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.
Bioorg Med Chem Lett 17: 2992-7 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Ligand based virtual screening and biological evaluation of inhibitors of chorismate mutase (Rv1885c) from Mycobacterium tuberculosis H37Rv.
Bioorg Med Chem Lett 17: 3053-8 (2007)
Central Drug Research Institute
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 17: 2966-70 (2007)
F. Hoffmann-La Roche
Evidence for a novel binding site conformer of aldose reductase in ligand-bound state.
J Mol Biol 369: 186-97 (2007)
University Of Marburg
A refined pharmacophore identifies potent 4-amino-7-chloroquinoline-based inhibitors of the botulinum neurotoxin serotype A metalloprotease.
J Med Chem 50: 2127-36 (2007)
National Cancer Institute At Frederick
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.
Bioorg Med Chem 15: 4175-92 (2007)
Astellas Pharma
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Bioorg Med Chem 15: 3635-48 (2007)
Wyeth Research
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
Bioorg Med Chem Lett 17: 3473-9 (2007)
Tanabe Research Laboratories Usa
Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.
Bioorg Med Chem Lett 17: 2921-6 (2007)
China Pharmaceutical University
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.
Bioorg Med Chem Lett 17: 3130-5 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques.
J Med Chem 50: 2157-65 (2007)
University Of Pennsylvania
Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors.
J Med Chem 50: 2060-6 (2007)
Eberhard-Karls-University T£Bingen
Beta-substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core.
Bioorg Med Chem Lett 17: 3146-51 (2007)
Merck Frosst Centre For Therapeutic Research
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
J Med Chem 50: 2200-12 (2007)
Amgen
Novel series of substituted biphenylmethyl urea derivatives as MCH-R1 antagonists for the treatment of obesity.
Bioorg Med Chem 15: 3896-911 (2007)
University Of Navarra
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Bioorg Med Chem 15: 3649-60 (2007)
Janssen-Cilag
PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta).
Bioorg Med Chem Lett 17: 2728-30 (2007)
Inha University
Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor.
Bioorg Med Chem Lett 17: 3117-21 (2007)
Wyeth Research
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
J Med Chem 50: 2254-8 (2007)
Harvard Medical School
Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor.
J Med Chem 50: 2030-9 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
Mechanisms for picrotoxinin and picrotin blocks of alpha2 homomeric glycine receptors.
J Biol Chem 282: 16016-35 (2007)
Université
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
Antimicrob Agents Chemother 51: 2078-84 (2007)
Emory University
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
J Biol Chem 282: 17314-24 (2007)
Consiglio Nazionale Delle Ricerche
Interaction between HIV-1 Rev and integrase proteins: a basis for the development of anti-HIV peptides.
J Biol Chem 282: 15743-53 (2007)
The Hebrew University Of Jerusalem
Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.
J Med Chem 50: 2144-56 (2007)
University Of Missouri-Columbia
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.
J Med Chem 50: 2067-77 (2007)
Salk Institute
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.
J Med Chem 50: 2269-72 (2007)
Bristol-Myers Squibb
Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit.
Bioorg Med Chem 15: 3684-91 (2007)
Texas A&M University
Polyphenols based on isoflavones as inhibitors of Helicobacter pylori urease.
Bioorg Med Chem 15: 3703-10 (2007)
Nanjing University
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.
Bioorg Med Chem Lett 17: 3048-52 (2007)
Kyoto Pharmaceutical University
PDE-10A inhibitors as insulin secretagogues.
Bioorg Med Chem Lett 17: 2869-73 (2007)
Bayer Pharmaceuticals
Preparation of novel anthranilic acids as antibacterial agents: extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity.
Bioorg Med Chem Lett 17: 3113-6 (2007)
Pharmacia
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).
Bioorg Med Chem 15: 3854-68 (2007)
Université
Structure based de novo design of novel glycogen synthase kinase 3 inhibitors.
Bioorg Med Chem 15: 3728-36 (2007)
Addis Ababa University
3-{2-[Bis-(4-fluorophenyl)methoxy]ethyl}-6-substituted-3,6-diazabicyclo[3.1.1]heptanes as novel potent dopamine uptake inhibitors.
Bioorg Med Chem 15: 3748-55 (2007)
Universit£
R-isomers of Arg-Gly-Asp (RGD) mimics as potent alphavbeta3 inhibitors.
Bioorg Med Chem 15: 3783-800 (2007)
Pfizer
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.
Bioorg Med Chem 15: 3801-17 (2007)
St. Jude Children'S Research Hospital
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.
Bioorg Med Chem Lett 17: 3072-6 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.
Bioorg Med Chem Lett 17: 3081-6 (2007)
Pfizer
Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.
Bioorg Med Chem Lett 17: 3077-80 (2007)
Ucb Pharma
Cellular characterization of a novel focal adhesion kinase inhibitor.
J Biol Chem 282: 14845-52 (2007)
University Of Virginia
Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII.
J Biol Chem 282: 15208-16 (2007)
University Of Wisconsin
Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
Bioorg Med Chem 15: 3883-8 (2007)
Kyushu University
Small molecule antagonists of the CC chemokine receptor 4 (CCR4).
Bioorg Med Chem Lett 17: 3141-5 (2007)
Millennium Pharmaceuticals
4-substituted indazoles as new inhibitors of neuronal nitric oxide synthase.
Bioorg Med Chem Lett 17: 3177-80 (2007)
Upres-Ea 3915
Methylenebis(sulfonamide) linked nicotinamide adenine dinucleotide analogue as an inosine monophosphate dehydrogenase inhibitor.
Bioorg Med Chem Lett 17: 3152-5 (2007)
University Of Minnesota
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Bioorg Med Chem Lett 17: 2697-702 (2007)
Merck Research Laboratories
Development of molecular probes for second-site screening and design of protein tyrosine phosphatase inhibitors.
J Med Chem 50: 2137-43 (2007)
Institute For Medical Research
Identification of novel fragment compounds targeted against the pY pocket of v-Src SH2 by computational and NMR screening and thermodynamic evaluation.
Proteins 67: 981-90 (2007)
University College London
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
Bioorg Med Chem 15: 3368-72 (2007)
University Of Chile
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.
Bioorg Med Chem 15: 3321-33 (2007)
Wyeth Research
Discovery of a novel small molecule binding site of human survivin.
Bioorg Med Chem Lett 17: 3122-9 (2007)
Abbott Laboratories
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.
Bioorg Med Chem Lett 17: 3099-104 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 17: 3136-40 (2007)
Abbott Laboratories
Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia.
Proc Natl Acad Sci U S A 104: 6061-5 (2007)
University Of Minnesota
Habbemines A and B, pyrrolidine alkaloids with human delta-opioid receptor binding affinity from the leaves of Elaeocarpus habbemensis.
J Nat Prod 70: 866-8 (2007)
Griffith University
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization.
Bioorg Med Chem 15: 3390-412 (2007)
Pfizer
Phenolic hydrazones are potent inhibitors of macrophage migration inhibitory factor proinflammatory activity and survival improving agents in sepsis.
J Med Chem 50: 1993-7 (2007)
The New York School Of Medicine
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
Bioorg Med Chem Lett 17: 3208-11 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
Bioorg Med Chem Lett 17: 3109-12 (2007)
Pfizer
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity.
Bioorg Med Chem Lett 17: 2706-11 (2007)
Bayer Healthcare
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S.
Bioorg Med Chem Lett 17: 2899-903 (2007)
Gnf
Neuroprotective principles from Gastrodia elata.
J Nat Prod 70: 571-4 (2007)
National Research Institute Of Chinese Medicine
Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters.
J Med Chem 50: 1850-64 (2007)
University Of Alberta
Synthesis and SAR studies of a novel class of S1P1 receptor antagonists.
Bioorg Med Chem 15: 3548-64 (2007)
Sankyo
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
Bioorg Med Chem 15: 3450-6 (2007)
Institute Of Biological Chemistry And The Genomics Research Center
Design of potent PPARalpha agonists.
Bioorg Med Chem Lett 17: 3198-202 (2007)
Novo Nordisk
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.
Bioorg Med Chem Lett 17: 2465-9 (2007)
Boehringer Ingelheim Pharmaceuticals
Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates.
Bioorg Med Chem Lett 17: 3212-6 (2007)
Université
Fluorinated NSC as a Cdc25 inhibitor.
Bioorg Med Chem Lett 17: 2351-4 (2007)
Sejong University
Covalent reactions of wortmannin under physiological conditions.
Chem Biol 14: 321-8 (2007)
Massachusetts General Hospital
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.
J Nat Prod 70: 859-62 (2007)
Tahitian Noni International
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
J Med Chem 50: 1876-85 (2007)
St. Jude Research Hospital
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
J Med Chem 50: 1723-6 (2007)
University Of Michigan
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
J Med Chem 50: 1810-27 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines.
Bioorg Med Chem 15: 3499-504 (2007)
Inha University
Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors.
Bioorg Med Chem 15: 3524-38 (2007)
The Danish University Of Pharmaceutical Sciences
Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails.
Bioorg Med Chem Lett 17: 2685-91 (2007)
Ecole Nationale Sup£Rieure De Chimie De Montpellier
Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.
Bioorg Med Chem Lett 17: 2712-7 (2007)
Nippon Shinyaku
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
Bioorg Med Chem Lett 17: 2372-5 (2007)
Birla Institute Of Technology And Science
ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents.
Eur J Pharmacol 562: 1-11 (2007)
The Hebrew University Of Jerusalem
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
J Med Chem 50: 1988-92 (2007)
University Of Copenhagen
Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.
J Med Chem 50: 1939-57 (2007)
University Of Montpellier
NMR screening applied to the fragment-based generation of inhibitors of creatine kinase exploiting a new interaction proximate to the ATP binding site.
J Med Chem 50: 1865-75 (2007)
Universit£
Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens.
Bioorg Med Chem 15: 3445-9 (2007)
Nippon Suisan Kaisha
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.
J Med Chem 50: 2213-24 (2007)
Astrazeneca
Inhibitory effect on soybean lipoxygenase and docking studies of some secondary metabolites, isolated from Origanum vulgare L. ssp. hirtum.
J Enzyme Inhib Med Chem 22: 99-104 (2007)
University Of Athens
The nucleoside analog sangivamycin induces apoptotic cell death in breast carcinoma MCF7/adriamycin-resistant cells via protein kinase Cdelta and JNK activation.
J Biol Chem 282: 15271-83 (2007)
Georgetown University Medical Center
Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism.
J Biol Chem 282: 15799-811 (2007)
University Of Copenhagen
Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives.
Antimicrob Agents Chemother 51: 2123-9 (2007)
Instituto De Parasitolog£A Y Biomedicina&Quot;L£Pez-Neyra
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr
Drug Metab Dispos 35: 929-36 (2007)
Targegen
Examination of acylated 4-aminopiperidine-4-carboxylic acid residues in the phosphotyrosyl+1 position of Grb2 SH2 domain-binding tripeptides.
J Med Chem 50: 1978-82 (2007)
National Cancer Institute-Frederick
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.
J Med Chem 50: 1958-72 (2007)
Newcastle University
1-(1,3-Benzodioxol-5-ylmethyl)-3-[4-(1H-imidazol-1-yl)phenoxy]-piperidine analogs as potent and selective inhibitors of nitric oxide formation.
Bioorg Med Chem Lett 17: 2499-504 (2007)
Berlex Biosciences
Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies.
Bioorg Med Chem Lett 17: 2749-55 (2007)
Lucknow University
Structural and thermodynamic study on aldose reductase: nitro-substituted inhibitors with strong enthalpic binding contribution.
J Mol Biol 368: 618-38 (2007)
University Of Marburg
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bioorg Med Chem Lett 17: 2828-33 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.
Bioorg Med Chem Lett 17: 2760-4 (2007)
Inha University
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett 17: 2769-74 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.
Bioorg Med Chem Lett 17: 2355-60 (2007)
The Scripps Research Institute
Development of integrase inhibitors for treatment of AIDS: an overview.
Eur J Med Chem 42: 1159-68 (2007)
K.L.E.S. College Of Pharmacy
Structure-based discovery of new small molecule inhibitors of low molecular weight protein tyrosine phosphatase.
Eur J Med Chem 42: 1102-8 (2007)
Institute For Research In Biomedicine (Irb)
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
J Med Chem 50: 1983-7 (2007)
Abbott Laboratories
Nodulisporol and Nodulisporone, novel specific inhibitors of human DNA polymerase lambda from a fungus, Nodulisporium sp.
Bioorg Med Chem 15: 3109-14 (2007)
Science University Of Tokyo
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
J Med Chem 50: 1727-30 (2007)
Johnson & Johnson Pharmaceutical Research And Development
c-Src protein kinase inhibitors block assembly and maturation of dengue virus.
Proc Natl Acad Sci U S A 104: 3520-5 (2007)
Harvard Medical School
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
Proc Natl Acad Sci U S A 104: 3456-9 (2007)
The Johns Hopkins University School Of Medicine
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.
Proc Natl Acad Sci U S A 104: 4106-11 (2007)
Millennium Pharmaceuticals
Synthesis and evaluation of transthyretin amyloidosis inhibitors containing carborane pharmacophores.
Proc Natl Acad Sci U S A 104: 4808-13 (2007)
University Of California
Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b.
J Med Chem 50: 1445-8 (2007)
Arena Pharmaceuticals
Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor.
J Med Chem 50: 1711-5 (2007)
Uppsala University
SCO-1, a novel plasmid-mediated class A beta-lactamase with carbenicillinase characteristics from Escherichia coli.
Antimicrob Agents Chemother 51: 2185-8 (2007)
Institut Pasteur Hellenique
Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
J Med Chem 50: 1610-7 (2007)
University Of Copenhagen
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.
J Med Chem 50: 1514-27 (2007)
Abbott Laboratories
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).
J Med Chem 50: 1693-7 (2007)
Via Zambeletti 25
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).
J Med Chem 50: 1571-83 (2007)
Via Zambeletti 25
Self-organizing maps for identification of new inhibitors of P-glycoprotein.
J Med Chem 50: 1698-702 (2007)
University Of Vienna
Fluorogenic probes for monitoring peptide binding to class II MHC proteins in living cells.
Nat Chem Biol 3: 222-8 (2007)
University Of Massachusetts Medical School
The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain.
J Biol Chem 282: 13395-401 (2007)
Stanford University
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.
Bioorg Med Chem Lett 17: 2879-85 (2007)
Merck Research Laboratories
Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel.
Bioorg Med Chem Lett 17: 2849-53 (2007)
Icagen
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Bioorg Med Chem Lett 17: 2171-8 (2007)
Neurocrine Biosciences
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Bioorg Med Chem Lett 17: 2886-9 (2007)
Amgen
Synthesis of fluorescent-labeled aeruginosin derivatives for high-throughput fluorescence correlation spectroscopy assays.
Bioorg Med Chem Lett 17: 2904-7 (2007)
Graduate School Of Science And Engineering
Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Bioorg Med Chem Lett 17: 2656-60 (2007)
Adolor
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.
Bioorg Med Chem 15: 3235-40 (2007)
Hokkaido University
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.
Bioorg Med Chem 15: 3161-70 (2007)
Universit£
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.
Bioorg Med Chem Lett 17: 2863-8 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 17: 2838-43 (2007)
University Of Edinburgh
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.
Bioorg Med Chem Lett 17: 2817-22 (2007)
Abbott Laboratories
Synthesis of enantiomerically pure milnacipran analogs and inhibition of dopamine, serotonin, and norepinephrine transporters.
Bioorg Med Chem Lett 17: 2834-7 (2007)
University Of Oslo
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Bioorg Med Chem Lett 17: 2365-71 (2007)
Abbott Laboratories
3D-QSAR and molecular docking studies on benzothiazole derivatives as Candida albicans N-myristoyltransferase inhibitors.
Eur J Med Chem 42: 477-86 (2007)
Second Military Medical University
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
Cancer Cell 11: 217-27 (2007)
Harvard Medical School
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
J Med Chem 50: 1558-70 (2007)
University Walk
Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.
J Med Chem 50: 1973-7 (2007)
Sapienza University Of Rome
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
Bioorg Med Chem Lett 17: 2558-60 (2007)
Institute For Natural Product Research And Infection Biology
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.
Bioorg Med Chem Lett 17: 2430-3 (2007)
China Pharmaceutical University
Design and evaluation of 'Linkerless' hydroxamic acids as selective HDAC8 inhibitors.
Bioorg Med Chem Lett 17: 2874-8 (2007)
Ithaca College
Design, synthesis and melatoninergic activity of new unsubstituted and beta,beta'-difunctionalised 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-alkanamides.
Eur J Med Chem 42: 1004-13 (2007)
University Of Athens
Synthesis of valiolamine and some precursors for bioactive carbaglycosylamines from (-)-vibo-quercitol produced by biogenesis of myo-inositol.
J Nat Prod 70: 493-7 (2007)
Keio University
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
J Med Chem 50: 1651-7 (2007)
Griffith University
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
J Med Chem 50: 1584-97 (2007)
Abbott Laboratories
Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
J Med Chem 50: 1495-503 (2007)
Novo Nordisk
Nonprenylated rotenoids, a new class of potent breast cancer resistance protein inhibitors.
J Med Chem 50: 1933-8 (2007)
Umr 5086 Cnrs/Universit£
Structural and functional basis of cyclooxygenase inhibition.
J Med Chem 50: 1425-41 (2007)
Institute For Chemical Biology And Center In Molecular Toxicology
Heme oxygenase inhibition by 2-oxy-substituted 1-(1H-imidazol-1-yl)-4-phenylbutanes: effect of halogen substitution in the phenyl ring.
Bioorg Med Chem 15: 3225-34 (2007)
Queen'S University
Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.
Bioorg Med Chem 15: 3143-51 (2007)
University Of Cagliari
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.
Bioorg Med Chem Lett 17: 2438-42 (2007)
Astellas Pharma
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.
J Med Chem 50: 1546-57 (2007)
Gsk
Affinity-based ranking of ligands for DPP-4 from mixtures.
Bioorg Med Chem Lett 17: 2404-7 (2007)
Merck Research Laboratories
Potent and selective xanthine-based inhibitors of phosphodiesterase 5.
Bioorg Med Chem Lett 17: 2376-9 (2007)
Novartis Institutes Of Biomedical Research
Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
Bioorg Med Chem 15: 2935-43 (2007)
Princeton University
The rational design of inhibitors of nitric oxide formation by inducible nitric oxide synthase.
Bioorg Med Chem Lett 17: 2505-8 (2007)
Berlex Biosciences
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
Bioorg Med Chem Lett 17: 1875-8 (2007)
Yale University
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.
Bioorg Med Chem Lett 17: 2074-9 (2007)
National Institute On Drug Abuse
Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.
Bioorg Med Chem Lett 17: 2414-20 (2007)
Chinese Academy Of Sciences
Probing acid replacements of thiophene PTP1B inhibitors.
Bioorg Med Chem Lett 17: 2913-20 (2007)
Wyeth Research
Sulfonamide-related conformational effects and their importance in structure-based design.
Bioorg Med Chem Lett 17: 2931-4 (2007)
Glaxosmithkline
Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
J Med Chem 50: 1627-34 (2007)
Università
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.
J Med Chem 50: 1449-57 (2007)
Università
Inhibition of secreted phospholipase A2. 4-glycerol derivatives of 4,5-dihydro-3-(4-tetradecyloxybenzyl)-1,2,4-4H-oxadiazol-5-one with broad activities.
J Med Chem 50: 1618-26 (2007)
Université
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.
Nat Chem Biol 3: 229-38 (2007)
University Of California
Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors.
Bioorg Med Chem Lett 17: 2608-13 (2007)
Array Biopharma
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors.
Bioorg Med Chem Lett 17: 2622-8 (2007)
Korea Research Institute Of Chemical Technology
Bisphosphonates as inhibitors of Trypanosoma cruzi hexokinase: kinetic and metabolic studies.
J Biol Chem 282: 12377-87 (2007)
Instituto Venezolano De Investigaciones Cient£Ficas
Modeling of human ghrelin receptor (hGHS-R1a) in its close state and validation by molecular docking.
Bioorg Med Chem 15: 3054-64 (2007)
Universit£
N-(3-(4-Hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors.
Bioorg Med Chem Lett 17: 2448-51 (2007)
University Of Kuopio
Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists.
Bioorg Med Chem Lett 17: 2535-9 (2007)
Neurocrine Biosciences
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.
Bioorg Med Chem Lett 17: 2161-5 (2007)
University Of Arizona
Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.
J Med Chem 50: 1335-46 (2007)
University Of Hamburg
(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors.
J Med Chem 50: 1675-84 (2007)
Korea Research Institute Of Bioscience And Biotechnology
Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging.
J Med Chem 50: 1028-40 (2007)
University Of Illinois
Novel sigma receptor ligands: synthesis and biological profile.
J Med Chem 50: 951-61 (2007)
University Of Catania
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents.
J Med Chem 50: 1322-34 (2007)
University Of Lille
Acquired echinocandin resistance in a Candida krusei isolate due to modification of glucan synthase.
Antimicrob Agents Chemother 51: 1876-8 (2007)
Rutgers University
Morin (3,5,7,2',4'-pentahydroxyflavone) exhibits potent inhibitory actions on urate transport by the human urate anion transporter (hURAT1) expressed in human embryonic kidney cells.
Drug Metab Dispos 35: 981-6 (2007)
The Chinese University Of Hong Kong
Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.
J Biol Chem 282: 13033-46 (2007)
The Scripps Research Institute
Novel selective human mitochondrial kinase inhibitors: design, synthesis and enzymatic activity.
Bioorg Med Chem 15: 3065-81 (2007)
University Of Ferrara
Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations.
J Med Chem 50: 1241-53 (2007)
Sapienza University Of Rome
From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors.
J Med Chem 50: 1213-21 (2007)
Eberhard-Karls-University TüBingen
Identification, synthesis, and biological evaluation of novel pyrazoles as low molecular weight luteinizing hormone receptor agonists.
Bioorg Med Chem Lett 17: 2080-5 (2007)
Merck Serono
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
Eur J Med Chem 42: 993-1003 (2007)
Katholieke Universiteit Leuven
Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation.
Bioorg Med Chem 15: 2907-19 (2007)
University Of Montpellier
1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: bioisosteric replacement of the carboxylic acid and carboxamide moiety.
Bioorg Med Chem 15: 2883-91 (2007)
University Of MüNster
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
J Agric Food Chem 55: 2276-81 (2007)
University Of California
Calcitonin gene-related peptide analogues with aza and indolizidinone amino acid residues reveal conformational requirements for antagonist activity at the human calcitonin gene-related peptide 1 receptor.
J Med Chem 50: 1401-8 (2007)
Université
High-throughput screening for human lysosomal beta-N-Acetyl hexosaminidase inhibitors acting as pharmacological chaperones.
Chem Biol 14: 153-64 (2007)
Research Institute, Hospital For Sick Children
Acridone derivatives: design, synthesis, and inhibition of breast cancer resistance protein ABCG2.
Bioorg Med Chem 15: 2892-7 (2007)
Umr 5063 Cnrs/Universit£
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).
Bioorg Med Chem Lett 17: 2179-83 (2007)
Johnson & Johnson Pharmaceutical Research & Development
1,2,3-Triazolylalkylribitol derivatives as nucleoside hydrolase inhibitors.
Bioorg Med Chem Lett 17: 2523-6 (2007)
University Of Antwerp
Sesterterpene sulfates as isocitrate lyase inhibitors from tropical sponge Hippospongia sp.
Bioorg Med Chem Lett 17: 2483-6 (2007)
Korea Ocean Research And Development Institute
Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors.
Bioorg Med Chem Lett 17: 2603-7 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and in vitro evaluation of tetrahydroisoquinolinyl benzamides as ligands for sigma receptors.
Bioorg Med Chem Lett 17: 2594-7 (2007)
University Of Missouri-Columbia
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 17: 2123-5 (2007)
Sun Yat-Sen University
M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: serominic compounds.
Bioorg Med Chem Lett 17: 2649-55 (2007)
University Of Strathclyde
Optimization of halopemide for phospholipase D2 inhibition.
Bioorg Med Chem Lett 17: 2310-1 (2007)
Novartis Institutes For Biomedical Research
Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).
Bioorg Med Chem Lett 17: 2317-21 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.
Bioorg Med Chem Lett 17: 2531-4 (2007)
Johnson And Johnson Pharmaceutical Research And Development
Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors.
Bioorg Med Chem Lett 17: 2540-4 (2007)
Neuraxon
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors.
Bioorg Med Chem Lett 17: 2618-21 (2007)
Mitsubishi Pharma
Relationship between quantum-chemical descriptors of proton dissociation and experimental acidity constants of various hydroxylated coumarins. Identification of the biologically active species for xanthine oxidase inhibition.
Eur J Med Chem 42: 1028-31 (2007)
Università
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
Eur J Med Chem 42: 1044-8 (2007)
Sungshin Women'S University
Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.
Eur J Med Chem 42: 799-806 (2007)
University Of Patras
Generation of oxamic acid libraries: antimalarials and inhibitors of Plasmodium falciparum lactate dehydrogenase.
J Comb Chem 9: 292-300 (2007)
University Of Mississippi
Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors.
J Med Chem 50: 1146-57 (2007)
Berlex Biosciences
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.
J Med Chem 50: 1365-79 (2007)
Pharmaceutical Research Institute
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
J Med Chem 50: 1414-7 (2007)
Clinical Research Institute Of Montreal
Somatostatin receptor-binding peptides suitable for tumor radiotherapy with Re-188 or Re-186. Chemistry and initial biological studies.
J Med Chem 50: 1354-64 (2007)
Diatide Research Laboaratories
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase.
J Med Chem 50: 1124-32 (2007)
Astex
Application of fragment screening by X-ray crystallography to beta-secretase.
J Med Chem 50: 1116-23 (2007)
Astex
Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells.
J Med Chem 50: 1635-44 (2007)
The Ohio State University
Homology modeling of human Fyn kinase structure: discovery of rosmarinic acid as a new Fyn kinase inhibitor and in silico study of its possible binding modes.
J Med Chem 50: 1090-100 (2007)
Glaxosmithkline
Phosph(on)ate as a zinc-binding group in metalloenzyme inhibitors: X-ray crystal structure of the antiviral drug foscarnet complexed to human carbonic anhydrase I.
Bioorg Med Chem Lett 17: 2210-5 (2007)
Universit£
2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.
Bioorg Med Chem Lett 17: 2643-8 (2007)
Merck Sharp And Dohme Research Laboratories
CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives.
Bioorg Med Chem Lett 17: 1883-7 (2007)
Berlex Biosciences
Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.
Bioorg Med Chem Lett 17: 2492-8 (2007)
Vrije Universiteit Brussel
Guanidinylated neomycin delivers large, bioactive cargo into cells through a heparan sulfate-dependent pathway.
J Biol Chem 282: 13585-91 (2007)
University Of California
Identification of anesthetic binding sites on human serum albumin using a novel etomidate photolabel.
J Biol Chem 282: 12038-47 (2007)
Imperial College
Identification of nonpeptide CCR5 receptor agonists by structure-based virtual screening.
J Med Chem 50: 1294-303 (2007)
Cnrs Umr 7175-Lc1
N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
J Med Chem 50: 1222-30 (2007)
Universit£
Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila.
Antimicrob Agents Chemother 51: 2136-42 (2007)
Universit£
Novel malonamide derivatives as potent kappa opioid receptor agonists.
Bioorg Med Chem Lett 17: 1951-5 (2007)
Adolor
Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid.
Bioorg Med Chem Lett 17: 2216-9 (2007)
Wayne State University
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
Bioorg Med Chem Lett 17: 2566-9 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage.
Bioorg Med Chem 15: 2573-86 (2007)
Università
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor.
Bioorg Med Chem 15: 2514-27 (2007)
Universit£
Pharmacophore modeling and in silico screening for new KDR kinase inhibitors.
Bioorg Med Chem Lett 17: 2126-33 (2007)
Shanghai Jiao Tong University
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
J Med Chem 50: 1380-400 (2007)
Wyeth Research
Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.
Bioorg Med Chem 15: 2533-43 (2007)
Università
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.
Bioorg Med Chem Lett 17: 2134-8 (2007)
Roche Research Center
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
Bioorg Med Chem Lett 17: 2150-5 (2007)
Pfizer
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
Bioorg Med Chem Lett 17: 2229-32 (2007)
University Of Mississippi
Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors.
Bioorg Med Chem Lett 17: 2118-22 (2007)
Chinese Academy Of Sciences
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
J Med Chem 50: 1166-76 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
Rational design of novel, potent small molecule pan-selectin antagonists.
J Med Chem 50: 1101-15 (2007)
Revotar Biopharmaceuticals
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
J Med Chem 50: 1280-7 (2007)
Vertex Pharmaceuticals
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
J Med Chem 50: 865-76 (2007)
Pierre Fabre Research Center
N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[(131)I]iodo-5-me thoxybenzyl)acetamide: a potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain.
J Med Chem 50: 848-55 (2007)
National Institute Of Radiological Sciences
Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
J Med Chem 50: 835-47 (2007)
University Of Montpellier
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
J Med Chem 50: 828-34 (2007)
Leiden/Amsterdam Center For Drug Research
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
J Med Chem 50: 794-806 (2007)
Merck Frosst Canada
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
J Med Chem 50: 776-81 (2007)
Elan Pharmaceuticals
Inhibitors of bacterial cystathionine beta-lyase: leads for new antimicrobial agents and probes of enzyme structure and function.
J Med Chem 50: 755-64 (2007)
Mcmaster University
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
J Med Chem 50: 1078-82 (2007)
Abbott Laboratories
Synthesis and preliminary evaluation of 18F- or 11C-labeled bicyclic nucleoside analogues as potential probes for imaging varicella-zoster virus thymidine kinase gene expression using positron emission tomography.
J Med Chem 50: 1041-9 (2007)
Ku Leuven
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
J Med Chem 50: 932-9 (2007)
Tokyo Medical And Dental University
Amphipathic benzoic acid derivatives: synthesis and binding in the hydrophobic tunnel of the zinc deacetylase LpxC.
Bioorg Med Chem 15: 2617-23 (2007)
University Of San Francisco
TRPM8 voltage sensor mutants reveal a mechanism for integrating thermal and chemical stimuli.
Nat Chem Biol 3: 174-82 (2007)
Ku Leuven
An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists.
Proc Natl Acad Sci U S A 104: 2602-7 (2007)
The Scripps Research Institute
3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.
J Mol Graph Model 26: 236-45 (2007)
Dalian University
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration.
Bioorg Med Chem 15: 2631-50 (2007)
Minase Research Institute
Dibenzothiazoles as novel amyloid-imaging agents.
Bioorg Med Chem 15: 2789-96 (2007)
Case Western Reserve University
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Bioorg Med Chem Lett 17: 2184-7 (2007)
Merck Research Laboratories
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV.
Bioorg Med Chem 15: 2715-35 (2007)
Minase Research Institute
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.
Bioorg Med Chem 15: 2587-600 (2007)
University Of Tokyo
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.
Bioorg Med Chem Lett 17: 1860-4 (2007)
Pharmaceutical Research Institute
A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice.
Bioorg Med Chem Lett 17: 1916-9 (2007)
Bayer Pharmaceuticals
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Bioorg Med Chem Lett 17: 2312-6 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease.
Bioorg Med Chem 15: 2601-10 (2007)
Dr. Reddys Laboratories
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.
Bioorg Med Chem Lett 17: 1903-7 (2007)
Merck Research Laboratories
Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.
J Nat Prod 70: 353-60 (2007)
University Of Bonn
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
J Med Chem 50: 901-14 (2007)
Gedeon Richter
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.
Bioorg Med Chem Lett 17: 1843-9 (2007)
Tibotec
Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics.
Bioorg Med Chem Lett 17: 2329-33 (2007)
Universit£
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Bioorg Med Chem Lett 17: 2322-8 (2007)
Merck Research Laboratories
Quantitative structure-selectivity relationship for M2 selectivity between M1 and M2 of piperidinyl piperidine derivatives as muscarinic antagonists.
Bioorg Med Chem Lett 17: 2260-6 (2007)
Shanghai Jiao Tong University School Of Medicine
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Bioorg Med Chem Lett 17: 2281-4 (2007)
Schering-Plough Research Institute
Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides.
Bioorg Med Chem Lett 17: 2250-3 (2007)
Vertex Pharmaceuticals
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Bioorg Med Chem 15: 2759-67 (2007)
Abbott Laboratories
Design, synthesis, inhibitory activity, and SAR studies of pyrrolidine derivatives as neuraminidase inhibitors.
Bioorg Med Chem 15: 2749-58 (2007)
Shandong University
Synthesis and characterization of a platinum(II) complex tethered to a ligand of the peripheral benzodiazepine receptor.
J Med Chem 50: 1019-27 (2007)
Università
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.
J Med Chem 50: 962-78 (2007)
National Cancer Institute-Frederick
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
Bioorg Med Chem Lett 17: 2305-9 (2007)
Amgen
Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius.
J Nat Prod 70: 296-9 (2007)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase.
J Med Chem 50: 1058-68 (2007)
The Scripps Research Institute
Mechanism of inactivation of plasminogen activator inhibitor-1 by a small molecule inhibitor.
J Biol Chem 282: 9288-96 (2007)
University Of Michigan Medical School
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
Bioorg Med Chem Lett 17: 2293-8 (2007)
University Of London
High-affinity carbamate analogues of morphinan at opioid receptors.
Bioorg Med Chem Lett 17: 1508-11 (2007)
Harvard Medical School
From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists.
Bioorg Med Chem Lett 17: 2254-9 (2007)
Glaxosmithkline
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.
Bioorg Med Chem Lett 17: 2299-304 (2007)
Amgen
Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 17: 1520-2 (2007)
University Of Florida
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Bioorg Med Chem Lett 17: 1865-70 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.
Bioorg Med Chem 15: 2312-21 (2007)
Universit£
Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates.
Bioorg Med Chem 15: 2298-311 (2007)
Universit£
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
Bioorg Med Chem Lett 17: 1956-60 (2007)
Universit£
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Bioorg Med Chem Lett 17: 2005-12 (2007)
Abbott Laboratories
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
Bioorg Med Chem Lett 17: 1996-9 (2007)
Pfizer
Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.
Bioorg Med Chem Lett 17: 2068-73 (2007)
Yale University
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.
Bioorg Med Chem Lett 17: 1773-8 (2007)
Glaxosmithkline
A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera.
J Mol Biol 367: 882-94 (2007)
Astex
The effect of 5-substitution in the pyrimidine ring of dUMP on the interaction with thymidylate synthase: molecular modeling and QSAR.
Bioorg Med Chem 15: 2346-58 (2007)
Polish Academy Of Sciences
Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells.
Bioorg Med Chem 15: 2269-82 (2007)
Equipe De Chimie ThéRapeutique
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.
Bioorg Med Chem 15: 2223-68 (2007)
Pomona College
Synthesis and biological evaluation of unprecedented classes of spiro-beta-lactams and azido-beta-lactams as acyl-CoA:cholesterol acyltransferase inhibitors.
Bioorg Med Chem Lett 17: 1946-50 (2007)
Università
Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
J Med Chem 50: 984-1000 (2007)
Bayer Healthcare Pharmaceuticals
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.
Bioorg Med Chem Lett 17: 2031-5 (2007)
Merck Research Laboratories
Novel hydroxamic acid-related phosphinates: inhibition of neutral aminopeptidase N (APN).
Bioorg Med Chem Lett 17: 1516-9 (2007)
Wroclaw University Of Technology
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bioorg Med Chem Lett 17: 2036-42 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Abeta fibril formation.
Bioorg Med Chem Lett 17: 1466-70 (2007)
Korea Institute Of Science And Technology
Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis.
J Med Chem 50: 940-50 (2007)
Dartmouth College
Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases.
Bioorg Med Chem 15: 2368-74 (2007)
Clermont Auvergne University
Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.
Bioorg Med Chem 15: 2375-85 (2007)
Taisho Pharmaceutical
Synthesis and evaluation of 2',4',6'-trihydroxychalcones as a new class of tyrosinase inhibitors.
Bioorg Med Chem 15: 2396-402 (2007)
Hokkaido University
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.
Bioorg Med Chem Lett 17: 1961-5 (2007)
Abbott Laboratories
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
Bioorg Med Chem Lett 17: 1527-31 (2007)
Ligand Pharmaceuticals
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.
Bioorg Med Chem Lett 17: 2022-5 (2007)
Pfizer
Oxazolidinones as novel human CCR8 antagonists.
Bioorg Med Chem Lett 17: 1722-5 (2007)
Glaxosmithkline
Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.
J Med Chem 50: 566-84 (2007)
Millennium Pharmaceuticals
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
J Med Chem 50: 512-20 (2007)
Medical University
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
J Med Chem 50: 489-500 (2007)
Friedrich-Alexander University
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.
J Med Chem 50: 462-71 (2007)
University Of Minnesota Health Science Center
Pharmacophore-based design of sphingosine 1-phosphate-3 receptor antagonists that include a 3,4-dialkoxybenzophenone scaffold.
J Med Chem 50: 442-54 (2007)
Toa Eiyo
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a.
J Med Chem 50: 433-41 (2007)
Cephalon
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.
J Med Chem 50: 429-32 (2007)
Amgen
Monoamine oxidase isoform-dependent tautomeric influence in the recognition of 3,5-diaryl pyrazole inhibitors.
J Med Chem 50: 425-8 (2007)
Sapienza University Of Rome
Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.
J Med Chem 50: 595-8 (2007)
Universita' Di Siena
Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR).
J Med Chem 50: 765-75 (2007)
National Institute Of Immunology
Potentiation of mammary cancer inhibition by combination of antagonists of growth hormone-releasing hormone with docetaxel.
Proc Natl Acad Sci U S A 104: 1943-6 (2007)
Veterans Affairs Medical Center
A clickable inhibitor reveals context-dependent autoactivation of p90 RSK.
Nat Chem Biol 3: 156-60 (2007)
University Of California
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.
Bioorg Med Chem 15: 1976-82 (2007)
Tehran University Of Medical Sciences
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt.
Bioorg Med Chem 15: 2441-52 (2007)
Abbott Laboratories
Probing binding requirements of NAD kinase with modified substrate (NAD) analogues.
Bioorg Med Chem Lett 17: 1512-5 (2007)
University Of Minnesota
An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes.
Bioorg Med Chem Lett 17: 2026-30 (2007)
Pharmaceutical Research Institute
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
Bioorg Med Chem Lett 17: 1471-4 (2007)
Johnson & Johnson Pharmaceutical Research & Development
A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening.
Bioorg Med Chem Lett 17: 1675-8 (2007)
Pfizer
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.
Bioorg Med Chem Lett 17: 1616-21 (2007)
Kyowa Hakko Kogyo
Carbonic anhydrase inhibitors. Inhibition of transmembrane isozymes XII (cancer-associated) and XIV with anions.
Bioorg Med Chem Lett 17: 1532-7 (2007)
Università
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
Bioorg Med Chem Lett 17: 1523-6 (2007)
Ligand Pharmaceuticals
Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.
Bioorg Med Chem Lett 17: 1558-61 (2007)
Nagoya City University
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.
Bioorg Med Chem Lett 17: 1788-92 (2007)
Merck Research Laboratories
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.
J Med Chem 50: 591-4 (2007)
Novartis Pharmaceuticals
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
J Med Chem 50: 603-6 (2007)
Incyte
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.
J Med Chem 50: 641-62 (2007)
Abbott Laboratories
New pyrrole inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity.
J Med Chem 50: 922-31 (2007)
Sapienza University Of Rome
Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter.
J Biol Chem 282: 8915-25 (2007)
University Of North Dakota School Of Medicine And Health Sciences
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
Bioorg Med Chem Lett 17: 1646-50 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity.
Bioorg Med Chem Lett 17: 2018-21 (2007)
Karo Bio
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors.
Bioorg Med Chem Lett 17: 1565-9 (2007)
Faculté
Saliniketals A and B, bicyclic polyketides from the marine actinomycete Salinispora arenicola.
J Nat Prod 70: 83-8 (2007)
University Of California - San Diego
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.
J Med Chem 50: 627-40 (2007)
Amgen
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
J Med Chem 50: 611-26 (2007)
Amgen
Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives.
J Med Chem 50: 707-12 (2007)
Universit?????? Degli Studi Di Roma "La Sapienza
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.
J Enzyme Inhib Med Chem 21: 703-10 (2006)
University Of Karachi
Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration.
J Biol Chem 282: 9740-7 (2007)
Cnrs-Commissariat à
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.
Bioorg Med Chem Lett 17: 1570-4 (2007)
Université
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Bioorg Med Chem Lett 17: 1679-83 (2007)
Valeant Pharmaceuticals Research And Development
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.
Bioorg Med Chem Lett 17: 1671-4 (2007)
Merck Frosst Centre For Therapeutic Research
Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.
Bioorg Med Chem Lett 17: 1718-21 (2007)
Pharmacopeia Drug Discovery
Cinnabaramides A-G: analogues of lactacystin and salinosporamide from a terrestrial streptomycete.
J Nat Prod 70: 246-52 (2007)
Intermed Discovery Gmbh (Imd)
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.
J Med Chem 50: 782-93 (2007)
University Of Nottingham
Synthesis and cell-based activity of a potent and selective protein tyrosine phosphatase 1B inhibitor prodrug.
J Med Chem 50: 856-64 (2007)
Purdue University
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
J Med Chem 50: 807-19 (2007)
Merck Research Laboratories
Structure-function analysis of Arg-Gly-Asp helix motifs in alpha v beta 6 integrin ligands.
J Biol Chem 282: 9657-65 (2007)
Cancer Research Uk Clinical Centre
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
J Med Chem 50: 607-10 (2007)
Amgen
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.
J Med Chem 50: 685-95 (2007)
Gsk
Chromosome-encoded narrow-spectrum Ambler class A beta-lactamase GIL-1 from Citrobacter gillenii.
Antimicrob Agents Chemother 51: 1365-72 (2007)
Bicetre Hospital
Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor.
Bioorg Med Chem Lett 17: 1584-9 (2007)
Gsk
Selective L-nitroargininylaminopyrrolidine and L-nitroargininylaminopiperidine neuronal nitric oxide synthase inhibitors.
Bioorg Med Chem 15: 1928-38 (2007)
Northwestern University
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.
Bioorg Med Chem Lett 17: 1691-4 (2007)
Virginia Commonwealth University
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
Bioorg Med Chem Lett 17: 1765-8 (2007)
Eli Lilly
Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists.
Bioorg Med Chem Lett 17: 1211-5 (2007)
Pharmacopeia Drug Discovery
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.
Bioorg Med Chem Lett 17: 1793-8 (2007)
Cephalon
Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.
Nature 445: 541-545 (2007)
The Scripps Research Institute
The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.
Bioorg Med Chem 15: 2092-105 (2007)
Procter & Gamble Pharmaceuticals
Identification of novel glycine sulfonamide antagonists for the EP1 receptor.
Bioorg Med Chem Lett 17: 1750-4 (2007)
Glaxosmithkline
Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.
Bioorg Med Chem Lett 17: 1713-7 (2007)
Glaxosmithkline
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
Bioorg Med Chem Lett 17: 1376-80 (2007)
Schering-Plough Research Institute
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.
Bioorg Med Chem 15: 1989-2005 (2007)
Taisho Pharmaceutical
Azetidinones as vasopressin V1a antagonists.
Bioorg Med Chem 15: 2054-80 (2007)
Lehigh University
Novel trifluoroacetophenone derivatives as malonyl-CoA decarboxylase inhibitors.
Bioorg Med Chem Lett 17: 1127-30 (2007)
Chugai Pharma Usa
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists.
Bioorg Med Chem Lett 17: 1659-62 (2007)
Schering-Plough Research Institute
Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines.
Bioorg Med Chem Lett 17: 1708-12 (2007)
Central Drug Research Institute
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
Bioorg Med Chem Lett 17: 1243-5 (2007)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of thienopyridines as Src-family selective Lck inhibitors.
Bioorg Med Chem Lett 17: 1167-71 (2007)
Abbott Bioresearch Center
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.
Bioorg Med Chem Lett 17: 1803-7 (2007)
Abbott Laboratories
1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.
Bioorg Med Chem Lett 17: 1741-5 (2007)
Glaxosmithkline
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Bioorg Med Chem Lett 17: 874-8 (2007)
Abbott Laboratories
Coupling substrate and ion binding to extracellular gate of a sodium-dependent aspartate transporter.
Nature 445: 387-93 (2007)
Columbia University
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
J Med Chem 50: 404-7 (2007)
Universita Di Pisa
Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.
J Med Chem 50: 399-403 (2007)
University Of Illinois At Urbana-Champaign
Synthesis and antimalarial activity of side chain modified 4-aminoquinoline derivatives.
J Med Chem 50: 394-8 (2007)
Central Drug Research Institute
Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation.
J Med Chem 50: 389-93 (2007)
Instituto De QuíMica MéDica
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
J Med Chem 50: 381-8 (2007)
Kochi Medical School
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.
J Med Chem 50: 374-80 (2007)
Universit£
Synthesis and cancer chemopreventive activity of zapotin, a natural product from Casimiroa edulis.
J Med Chem 50: 350-5 (2007)
Purdue University
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
J Med Chem 50: 344-9 (2007)
Pfizer
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
J Med Chem 50: 328-33 (2007)
Hungarian Academy Of Sciences
Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.
J Med Chem 50: 272-82 (2007)
Merck Research Laboratories
Optimization of monocarboxylate transporter 1 blockers through analysis and modulation of atropisomer interconversion properties.
J Med Chem 50: 254-63 (2007)
Astrazeneca
Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
J Med Chem 50: 233-40 (2007)
Eli Lilly
Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
J Med Chem 50: 219-32 (2007)
Massachusetts College Of Pharmacy And Health Sciences
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
J Med Chem 50: 199-210 (2007)
Achillion Pharmaceuticals
Structure-activity relationships of cyclic peptide-based chemokine receptor CXCR4 antagonists: disclosing the importance of side-chain and backbone functionalities.
J Med Chem 50: 192-8 (2007)
Kyoto University
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
J Med Chem 50: 186-91 (2007)
University Of Leeds
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
J Med Chem 50: 182-5 (2007)
Pfizer
Advances in development of dopaminergic aporphinoids.
J Med Chem 50: 171-81 (2007)
Chinese Academy Of Sciences
Development of selective inhibitors for anti-apoptotic Bcl-2 proteins from BHI-1.
Bioorg Med Chem 15: 2167-76 (2007)
University Of Minnesota
Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa.
Bioorg Med Chem 15: 2127-46 (2007)
Berlex
Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.
Eur J Nucl Med Mol Imaging 34: 1050-60 (2007)
Columbia University
Use of novel boronic acid transition state inhibitors to probe substrate affinity in SHV-type extended-spectrum beta-lactamases.
Antimicrob Agents Chemother 51: 1577-9 (2007)
Veterans Affairs Medical Center
Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase.
Mol Cancer Ther 6: 163-72 (2007)
Loma Linda University
Modulating effects of a novel skin-lightening agent, alpha-lipoic acid derivative, on melanin production by the formation of DOPA conjugate products.
Bioorg Med Chem 15: 1967-75 (2007)
Dhc
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
Bioorg Med Chem 15: 2156-66 (2007)
University Of North Carolina At Chapel Hill
Small-molecule agonists for the glucagon-like peptide 1 receptor.
Proc Natl Acad Sci U S A 104: 937-42 (2007)
Novo Nordisk Als
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.
Proc Natl Acad Sci U S A 104: 943-8 (2007)
National Center For Drug Screening
Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Bioorg Med Chem 15: 2187-97 (2007)
University Of Regensburg
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.
Bioorg Med Chem Lett 17: 1189-92 (2007)
Wyeth Research
Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).
Bioorg Med Chem Lett 17: 1185-8 (2007)
Wyeth Research
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Bioorg Med Chem Lett 17: 1386-91 (2007)
Merck
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
J Med Chem 50: 165-8 (2007)
University Of Arizona
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
J Med Chem 50: 149-64 (2007)
Abbott Laboratories
Metabolism-based identification of a potent thrombin receptor antagonist.
J Med Chem 50: 129-38 (2007)
Schering-Plough Research Institute
New beta-alanine derivatives are orally available glucagon receptor antagonists.
J Med Chem 50: 113-28 (2007)
Novo Nordisk
Isofagomine- and 2,5-anhydro-2,5-imino-D-glucitol-based glucocerebrosidase pharmacological chaperones for Gaucher disease intervention.
J Med Chem 50: 94-100 (2007)
The Scripps Research Institute
Discovering potassium channel blockers from synthetic compound database by using structure-based virtual screening in conjunction with electrophysiological assay.
J Med Chem 50: 83-93 (2007)
Chinese Academy Of Sciences
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
J Med Chem 50: 65-73 (2007)
University Of California San Francisco
2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists.
J Med Chem 50: 40-64 (2007)
Wyeth Research
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.
J Med Chem 50: 21-39 (2007)
Wyeth Research
Discovery and refinement of a new structural class of potent peptide deformylase inhibitors.
J Med Chem 50: 10-20 (2007)
Centre National De La Recherche Scientifique
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors.
J Med Chem 50: 6-9 (2007)
Glaxosmithkline
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.
J Med Chem 50: 2-5 (2007)
Glaxosmithkline
Structure and regulation of the human Nek2 centrosomal kinase.
J Biol Chem 282: 6833-42 (2007)
University Of Oxford
4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.
Bioorg Med Chem 15: 1586-605 (2007)
Abbott Laboratories
High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity.
Bioorg Med Chem Lett 17: 1280-3 (2007)
Harvard Medical School
Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold.
Bioorg Med Chem Lett 17: 1784-7 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.
Bioorg Med Chem Lett 17: 1233-7 (2007)
Bristol-Myers Squibb
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
Bioorg Med Chem Lett 17: 1254-9 (2007)
The Genomics Institute Of The Novartis Research Foundation
Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans.
Bioorg Med Chem Lett 17: 1221-5 (2007)
Sapienza University Of Rome
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
Bioorg Med Chem Lett 17: 1307-11 (2007)
F. Hoffmann-La Roche
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Bioorg Med Chem Lett 17: 1200-5 (2007)
Glaxosmithkline
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
Drug Metab Dispos 35: 493-500 (2007)
Act
Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones.
Bioorg Med Chem 15: 1651-8 (2007)
Ewha Womans University
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists.
Bioorg Med Chem 15: 1679-93 (2007)
Daiichi Pharmaceutical
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.
Bioorg Med Chem Lett 17: 1296-301 (2007)
Glaxosmithkline
3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.
Bioorg Med Chem Lett 17: 1274-9 (2007)
National Health Research Institutes
Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening.
Bioorg Med Chem Lett 17: 1422-7 (2007)
Institute Of Medical Research
A potent and orally active HIV-1 integrase inhibitor.
Bioorg Med Chem Lett 17: 1392-8 (2007)
Merck Research Laboratories
Cellular inhibition of protein tyrosine phosphatase 1B by uncharged thioxothiazolidinone derivatives.
Chembiochem 8: 179-86 (2007)
Mcgill University
Bioactive oligostilbenoids from the stem bark of Hopea exalata.
J Nat Prod 69: 1800-2 (2006)
Nanjing University
Sodwanone and yardenone triterpenes from a South African species of the marine sponge Axinella inhibit hypoxia-inducible factor-1 (HIF-1) activation in both breast and prostate tumor cells.
J Nat Prod 69: 1715-20 (2006)
University Of Mississippi
Hyrtiazepine, an azepino-indole-type alkaloid from the Red Sea marine sponge Hyrtios erectus.
J Nat Prod 69: 1676-9 (2006)
Umr 5154 Cnrs
Synthesis and biological evaluation of thiazolidine-2-one 1,1-dioxide as inhibitors of Escherichia coli beta-ketoacyl-ACP-synthase III (FabH).
Bioorg Med Chem Lett 17: 879-83 (2007)
Portland State University
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).
Bioorg Med Chem Lett 17: 1250-3 (2007)
Procter And Gamble Pharmaceuticals
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Bioorg Med Chem Lett 17: 1302-6 (2007)
F. Hoffmann-La Roche
3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors.
Bioorg Med Chem Lett 17: 1291-5 (2007)
Korea Research Institute Of Chemical Technology
3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa).
Bioorg Med Chem Lett 17: 1349-54 (2007)
Berlex Biosciences
Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides.
Bioorg Med Chem Lett 17: 1260-5 (2007)
University Of Nebraska Medical Center
Synthesis and HIV-1 integrase inhibitory activity of spiroundecane(ene) derivatives.
Bioorg Med Chem Lett 17: 1362-8 (2007)
Siberian Branch Of The Russian Academy Of Sciences
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Bioorg Med Chem 15: 1694-702 (2007)
Lanzhou University
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.
Bioorg Med Chem Lett 17: 1369-75 (2007)
Chemical Diversity
Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists.
Bioorg Med Chem Lett 17: 1399-402 (2007)
Friedrich-Schiller-UniversitäT Jena
Thienopyridine urea inhibitors of KDR kinase.
Bioorg Med Chem Lett 17: 1246-9 (2007)
Abbott Laboratories
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.
Bioorg Med Chem Lett 17: 925-31 (2007)
Mitsubishi Pharma
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Bioorg Med Chem Lett 17: 884-9 (2007)
Abbott Laboratories
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett 17: 1413-7 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.
Bioorg Med Chem Lett 17: 1358-61 (2007)
Wyeth Research
A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE.
Bioorg Med Chem Lett 17: 1408-12 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Carinatumins A-C, new alkaloids from Lycopodium carinatum inhibiting acetylcholinesterase.
Bioorg Med Chem 15: 1703-7 (2007)
Hoshi University
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.
Bioorg Med Chem Lett 17: 902-6 (2007)
Wyeth Research
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.
Bioorg Med Chem Lett 17: 974-7 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure of acid beta-glucosidase with pharmacological chaperone provides insight into Gaucher disease.
Nat Chem Biol 3: 101-7 (2007)
Harvard Medical School
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Proc Natl Acad Sci U S A 104: 270-5 (2007)
Genomics Institute Of The Novartis Research Foundation
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.
Eur J Med Chem 42: 334-43 (2007)
Johnson & Johnson Pharmaceutical Research And Development
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.
ACS Chem Biol 1: 702-12 (2006)
Rutgers University
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
J Med Chem 49: 7916-20 (2006)
University Of Michigan
Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors.
J Med Chem 49: 7912-5 (2006)
Eberhard-Karls-Universit£T
N,N'-Bisbenzylidenebenzene-1,4-diamines and N,N'-Bisbenzylidenenaphthalene-1,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors.
J Med Chem 49: 7907-11 (2006)
University Of Kuopio
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
J Med Chem 49: 7887-96 (2006)
Boehringer Ingelheim Pharmaceuticals
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.
J Med Chem 49: 7868-76 (2006)
Wyeth Research
Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.
J Med Chem 49: 7843-53 (2006)
Abbott Laboratories
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.
J Med Chem 49: 7826-35 (2006)
Dipartimento Di Scienze Farmaceutiche
9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
J Med Chem 49: 7816-25 (2006)
Westphalian Wilhelms-University
Synthesis and evaluation of multisubstrate bicyclic pyrimidine nucleoside inhibitors of human thymidine phosphorylase.
J Med Chem 49: 7807-15 (2006)
Attenuon
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.
J Med Chem 49: 7781-91 (2006)
Daiichi Asubio Medical Research Laboratories
N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
J Med Chem 49: 7766-73 (2006)
Instituto De QuíMica MéDica (Csic)
Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.
J Med Chem 49: 7731-9 (2006)
University Of Minnesota
Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization.
J Med Chem 49: 7697-710 (2006)
The Scripps Research Institute
2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity.
J Med Chem 49: 7683-96 (2006)
University Of Bath
Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo.
J Med Chem 49: 7636-45 (2006)
University Of Edinburgh
Antitubercular nucleosides that inhibit siderophore biosynthesis: SAR of the glycosyl domain.
J Med Chem 49: 7623-35 (2006)
University Of Minnesota
Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.
J Med Chem 49: 7607-10 (2006)
Laboratorio De Radicales Libres (Iqog, Csic)
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
J Med Chem 49: 7603-6 (2006)
Schering-Plough Research Institute
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
J Med Chem 49: 7596-9 (2006)
Bristol-Myers Squibb
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
J Med Chem 49: 7584-7 (2006)
Merck Research Laboratories
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.
J Biol Chem 282: 3428-32 (2007)
University Of Oklahoma Health Sciences Center
3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.
Bioorg Med Chem Lett 17: 1284-7 (2007)
Keimyung University
Quinazoline and benzimidazole MCH-1R antagonists.
Bioorg Med Chem Lett 17: 1403-7 (2007)
Argenta Discovery
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Bioorg Med Chem Lett 17: 916-20 (2007)
Glaxosmithkline
Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.
Bioorg Med Chem 15: 1533-8 (2007)
Sun Yat-Sen University
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
Bioorg Med Chem Lett 17: 1432-7 (2007)
Bristol-Myers Squibb
Novel amidino-substituted benzimidazoles: synthesis of compounds and inhibition of dipeptidyl peptidase III.
Bioorg Chem 35: 153-69 (2007)
The Josip Juraj Strossmayer University
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
Bioorg Med Chem Lett 17: 657-61 (2007)
Procter And Gamble Pharmaceuticals
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.
Bioorg Med Chem Lett 17: 1438-42 (2007)
Genentech
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
J Biol Chem 282: 8005-10 (2007)
Merck Research Laboratories
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.
Proc Natl Acad Sci U S A 103: 19866-71 (2006)
Targegen
Inhibitory effects of phloridzin dihydrate on the activity of mushroom (Agaricus bisporus) tyrosinase.
Bioorg Med Chem 15: 1568-71 (2007)
Xiamen University
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.
Bioorg Med Chem Lett 17: 907-10 (2007)
Johnson And Johnson Pharmaceutical Research And Development
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
Bioorg Med Chem Lett 17: 1443-6 (2007)
Abbott Laboratories
Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.
ACS Chem Biol 1: 585-93 (2006)
University Of California San Francisco
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.
ACS Chem Biol 1: 525-33 (2006)
Genentech
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors.
J Biol Chem 282: 5536-44 (2007)
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti
Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase.
J Biol Chem 282: 8368-79 (2007)
Chul
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
Bioorg Med Chem 15: 1828-47 (2007)
Organon Laboratories
High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis.
ACS Chem Biol 1: 43-53 (2006)
Suny Stony Brook
Antiparasitic drug nitazoxanide inhibits the pyruvate oxidoreductases of Helicobacter pylori, selected anaerobic bacteria and parasites, and Campylobacter jejuni.
Antimicrob Agents Chemother 51: 868-76 (2007)
University Of Virginia Health Systems
Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.
Bioorg Med Chem 15: 1212-28 (2007)
University Of Tennessee Health Science Center
Parallel solid synthesis of inhibitors of the essential cell division FtsZ enzyme as a new potential class of antibacterials.
Bioorg Med Chem 15: 1330-40 (2007)
Universit£
Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides.
Bioorg Med Chem Lett 17: 987-92 (2007)
Griffith University
Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.
Bioorg Med Chem Lett 17: 22-7 (2007)
Gsk
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
Bioorg Med Chem Lett 17: 937-41 (2007)
Lg Life Sciences
Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups--new classes of PPAR gamma/delta and PPAR alpha/gamma/delta agonists.
Bioorg Med Chem Lett 17: 1056-61 (2007)
Bayer Pharmaceuticals
Quantitative structure-activity relationship (QSAR) of indoloacetamides as inhibitors of human isoprenylcysteine carboxyl methyltransferase.
Bioorg Med Chem Lett 17: 1025-32 (2007)
National University Of Singapore
13C bis-labeled pyrroles: a tool for the identification of the rat metabolism of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester.
Bioorg Med Chem Lett 17: 969-73 (2007)
Glaxosmithkline
Synthesis of a novel inhibitor against MRSA and VRE: preparation from zerumbone ring opening material showing histidine-kinase inhibition.
Bioorg Med Chem Lett 17: 1098-101 (2007)
Kinki University
Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon.
Bioorg Med Chem Lett 17: 1112-6 (2007)
National Research Laboratory Of Lipid Metabolism And Atherosclerosis
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors.
Bioorg Med Chem Lett 17: 688-91 (2007)
Activesight
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
J Med Chem 49: 6888-96 (2006)
University Of Arizona
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
J Med Chem 49: 6869-87 (2006)
Abbott Laboratories
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.
J Med Chem 49: 6848-57 (2006)
Purdue University
Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole.
J Med Chem 49: 6833-40 (2006)
Universitat De Barcelona
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase i
J Med Chem 49: 6819-32 (2006)
Bristol-Myers Squibb
In silico-guided target identification of a scaffold-focused library: 1,3,5-triazepan-2,6-diones as novel phospholipase A2 inhibitors.
J Med Chem 49: 6768-78 (2006)
Cnrs Umr 7175
Synthesis, radiosynthesis, and biological evaluation of carbon-11 labeled 2beta-carbomethoxy-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.
J Med Chem 49: 6760-7 (2006)
Emory University
Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.
J Med Chem 49: 6726-31 (2006)
Abbott Laboratories
5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis.
J Med Chem 49: 6704-15 (2006)
University Hospital Of The WestfäLische Wilhelms-UniversitäT
Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.
J Med Chem 49: 6652-5 (2006)
University Of Southampton
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
J Med Chem 49: 6650-1 (2006)
Vrije Universiteit Amsterdam
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
J Med Chem 49: 6646-9 (2006)
Irbm-Mrl
Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.
J Med Chem 49: 6642-5 (2006)
University Of Bologna
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
J Med Chem 49: 6638-41 (2006)
7Tm Pharma
Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.
J Med Chem 49: 6635-7 (2006)
Karo Bio
Lead discovery and optimization of T-type calcium channel blockers.
Bioorg Med Chem 15: 1409-19 (2007)
Institute Of Science And Technology
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.
J Med Chem 49: 7549-53 (2006)
Eberhard-Karls University
Engineering of a VPAC2 receptor peptide agonist to impart dipeptidyl peptidase IV stability and enhance in vivo glucose disposal.
J Med Chem 49: 7545-8 (2006)
Bayer Pharmaceuticals
Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase.
J Med Chem 49: 7540-4 (2006)
Rheinische Friedrich-Wilhelms-Universitat Bonn
Design and evaluation of hydroxamate derivatives as metal-mediated inhibitors of a protein tyrosine kinase.
J Med Chem 49: 7532-9 (2006)
University Of Rhode Island
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
J Med Chem 49: 7513-7 (2006)
The University Of Texas
Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide.
J Med Chem 49: 7502-12 (2006)
Universit£
Structure-activity relationship analysis of the selective inhibition of transglutaminase 2 by dihydroisoxazoles.
J Med Chem 49: 7493-501 (2006)
Stanford University
Progressive docking: a hybrid QSAR/docking approach for accelerating in silico high throughput screening.
J Med Chem 49: 7466-78 (2006)
University Of British Columbia
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
J Med Chem 49: 7450-65 (2006)
Abbott Laboratories
High antiplasmodial activity of novel plasmepsins I and II inhibitors.
J Med Chem 49: 7440-9 (2006)
University Of Milan
Fluorinated conformationally restricted gamma-aminobutyric acid aminotransferase inhibitors.
J Med Chem 49: 7404-12 (2006)
Northwestern University
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
J Med Chem 49: 7373-83 (2006)
Ghent University
Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.
J Med Chem 49: 7366-72 (2006)
Orebro University
Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta.
J Med Chem 49: 7357-65 (2006)
Ghent University
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
J Med Chem 49: 7342-56 (2006)
University Of Massachusetts Medical School
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
J Med Chem 49: 7331-41 (2006)
University Of Illinois At Urbana - Champaign
Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition.
J Med Chem 49: 7307-16 (2006)
Albert-Ludwigs-University Of Freiburg
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
J Med Chem 49: 7290-306 (2006)
Adolor
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
J Med Chem 49: 7278-89 (2006)
Adolor
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
J Med Chem 49: 7270-3 (2006)
Merck Research Laboratories
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Antimicrob Agents Chemother 51: 543-50 (2007)
Gilead Sciences
The pyrophosphate analogue foscarnet traps the pre-translocational state of HIV-1 reverse transcriptase in a Brownian ratchet model of polymerase translocation.
J Biol Chem 282: 3337-46 (2007)
Mcgill University
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Bioorg Med Chem 15: 1237-51 (2007)
Kobe Gakuin University
Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects.
J Biol Chem 282: 2505-11 (2007)
Activx Biosciences
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
Bioorg Med Chem Lett 17: 662-7 (2007)
Ionix Pharmaceuticals
Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies.
J Biol Chem 282: 4085-93 (2007)
Johnson & Johnson Pharmaceutical
Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors.
J Biol Chem 282: 4094-101 (2007)
Johnson & Johnson Pharmaceutical
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
Bioorg Med Chem Lett 17: 1033-6 (2007)
Glaxosmithkline
Design and synthesis of a novel class of dual PPARgamma/delta agonists.
Bioorg Med Chem Lett 17: 1052-5 (2007)
Eli Lilly
Dibenzocyclooctadiene lignans: a class of novel inhibitors of multidrug resistance-associated protein 1.
Life Sci 80: 741-8 (2007)
Zhejiang University
Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors.
Bioorg Med Chem 15: 1311-22 (2007)
Procter & Gamble Pharmaceuticals
DAT/SERT selectivity of flexible GBR 12909 analogs modeled using 3D-QSAR methods.
Bioorg Med Chem 15: 1146-59 (2006)
University Heights
Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.
Bioorg Med Chem 15: 1266-74 (2007)
Instituto Superior T£Cnico
1,3-Disubstituted-imidazo[1,5-a]pyrazines as insulin-like growth-factor-I receptor (IGF-IR) inhibitors.
Bioorg Med Chem Lett 17: 1091-7 (2007)
Osi Pharmaceuticals
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
Bioorg Med Chem Lett 17: 1047-51 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Novel carbazole derivatives as NPY Y1 antagonists.
Bioorg Med Chem Lett 17: 1043-6 (2007)
Glaxosmithkline
Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides: a late-stage diversification approach to potent 5HT1B antagonists.
Bioorg Med Chem 15: 939-50 (2006)
Astrazeneca Pharmaceuticals
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
Bioorg Med Chem 15: 1394-408 (2007)
Chinese Academy Of Sciences
Design and study of some novel ibuprofen derivatives with potential nootropic and neuroprotective properties.
Bioorg Med Chem 15: 951-61 (2006)
Aristotelian University Of Thessaloniki
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.
Bioorg Med Chem 15: 1298-310 (2007)
University Of Kansas
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.
Bioorg Med Chem Lett 17: 587-92 (2007)
Merck Research Laboratories
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.
J Med Chem 49: 7247-51 (2006)
Nerviano Medical Sciences
Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.
J Med Chem 49: 7242-6 (2006)
Wayne State University
Discovering inhibitors of human sirtuin type 2: novel structural scaffolds.
J Med Chem 49: 7239-41 (2006)
University Of Kuopio
Structure-activity relationships of a novel series of urotensin II analogues: identification of a urotensin II antagonist.
J Med Chem 49: 7234-8 (2006)
University Of Rouen
Synthesis and radioligand binding studies of methoxylated 1,2,3,4-tetrahydroisoquinolinium derivatives as ligands of the apamin-sensitive Ca2+-activated K+ channels.
J Med Chem 49: 7208-14 (2006)
University Of Li£Ge
Discovery of a new class of macrocyclic antagonists to the human motilin receptor.
J Med Chem 49: 7190-7 (2006)
Tranzyme Pharma
Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.
J Med Chem 49: 7160-8 (2006)
Uppsala University
Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases.
J Med Chem 49: 7150-9 (2006)
Institute Of Organic And Bioorganic Chemistry
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).
J Med Chem 49: 7140-9 (2006)
Universit£
Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists.
J Med Chem 49: 7132-9 (2006)
Biogen Idec
Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
J Med Chem 49: 7119-31 (2006)
Biogen Idec
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.
J Med Chem 49: 7108-18 (2006)
Glaxosmithkline
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.
J Med Chem 49: 7095-107 (2006)
Glaxosmithkline
Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors.
J Med Chem 49: 7076-87 (2006)
University Of Bonn
Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones.
J Med Chem 49: 7063-75 (2006)
Teikyo University
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
J Med Chem 49: 7024-31 (2006)
Universite Montpellier Ii
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization.
J Med Chem 49: 6987-7001 (2006)
Human Biomolecular Research Institute
A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region.
J Med Chem 49: 6977-86 (2006)
University Of Prince Edward Island
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
J Med Chem 49: 6954-7 (2006)
Merck Research Laboratories
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors.
J Med Chem 49: 6950-3 (2006)
Central Pharmaceutical Research Institute
Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.
J Med Chem 49: 6946-9 (2006)
Cerep
Triterpene saponins from clematis mandshurica.
J Nat Prod 69: 1591-5 (2006)
Peking University Health Science Center
Biologically active triterpenoid saponins from Acanthopanax senticosus.
J Nat Prod 69: 1577-81 (2006)
Toho University
Protein tyrosine phosphatase-1B inhibitory activity of isoprenylated flavonoids isolated from Erythrina mildbraedii.
J Nat Prod 69: 1572-6 (2006)
Korea Research Institute Of Bioscience And Biotechnology
Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues.
Bioorg Med Chem 15: 702-13 (2006)
University Of Kansas
Synthesis of 11C-labelled (R)-OHDMI and CFMME and their evaluation as candidate radioligands for imaging central norepinephrine transporters with PET.
Bioorg Med Chem 15: 616-25 (2006)
Institutet
Serendipitous discovery of novel bacterial methionine aminopeptidase inhibitors.
Proteins 66: 538-46 (2007)
The Procter & Gamble Pharmaceuticals
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.
Bioorg Med Chem Lett 17: 315-9 (2007)
Boehringer Ingelheim Pharmaceuticals
Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.
Bioorg Med Chem Lett 17: 727-31 (2007)
Ono Pharmaceutical
Highly constrained bicyclic VLA-4 antagonists.
Bioorg Med Chem Lett 17: 597-601 (2007)
Merck Research Laboratories
Design and syntheses of novel phthalazin-1(2H)-one derivatives as acetohydroxyacid synthase inhibitors.
J Agric Food Chem 54: 9135-9 (2006)
Central China Normal University
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
Antimicrob Agents Chemother 51: 429-37 (2007)
Valeant Research And Development
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
Antimicrob Agents Chemother 51: 638-44 (2007)
Universidade Federal Do Rio De Janeiro
Substrate specificity analysis and inhibitor design of homoisocitrate dehydrogenase.
Bioorg Med Chem 15: 1346-55 (2007)
Tokyo Institute Of Technology
Forward chemical genetic approach identifies new role for GAPDH in insulin signaling.
Nat Chem Biol 3: 55-9 (2007)
New York University
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.
Proc Natl Acad Sci U S A 103: 18148-53 (2006)
Johns Hopkins University
Inhibition of Hsp90 with synthetic macrolactones: synthesis and structural and biological evaluation of ring and conformational analogs of radicicol.
Chem Biol 13: 1203-15 (2006)
University Of Nottingham
Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors.
Bioorg Med Chem 15: 1448-74 (2007)
Uppsala University
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Anal Biochem 360: 30-40 (2007)
Pfizer
High affinity Grb2-SH3 domain ligand incorporating Cbeta-substituted prolines in a Sos-derived decapeptide.
Bioorg Med Chem 15: 1439-47 (2007)
Université
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors.
Bioorg Med Chem 15: 641-55 (2006)
Mitsubishi Pharma
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
Bioorg Med Chem 15: 663-77 (2006)
University Of Virginia
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
Bioorg Med Chem Lett 17: 602-8 (2007)
Targegen
Solid-phase synthesis of Stat3 inhibitors incorporating O-carbamoylserine and O-carbamoylthreonine as glutamine mimics.
Bioorg Med Chem Lett 17: 654-6 (2007)
The University Of Texas
Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.
Bioorg Med Chem Lett 17: 1117-21 (2007)
Merck Research Laboratories
A review of anti-infective and anti-inflammatory chalcones.
Eur J Med Chem 42: 125-37 (2007)
Adam Mickiewicz University
Design, parallel synthesis and SAR of novel urotensin II receptor agonists.
Eur J Med Chem 42: 276-85 (2007)
G£Teborg University
TOMOCOMD-CARDD descriptors-based virtual screening of tyrosinase inhibitors: evaluation of different classification model combinations using bond-based linear indices.
Bioorg Med Chem 15: 1483-503 (2007)
Central University Of Las Villas
Structure-activity relationships of 19-norvitamin D analogs having a fluoroethylidene group at the C-2 position.
Bioorg Med Chem 15: 1475-82 (2007)
Tokyo Medical And Dental University
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.
Bioorg Med Chem 15: 903-14 (2006)
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand.
Bioorg Med Chem 15: 854-67 (2006)
Teikyo University
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.
Bioorg Med Chem Lett 17: 750-5 (2007)
Abbott Laboratories
New approaches to molecular cancer therapeutics.
Nat Chem Biol 2: 689-700 (2006)
The Institute Of Cancer Research
From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.
Bioorg Med Chem Lett 17: 350-3 (2007)
Irbm-Mrl Rome
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.
Bioorg Med Chem Lett 17: 702-6 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.
Bioorg Med Chem Lett 17: 668-72 (2007)
Abbott Laboratories
Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.
Bioorg Med Chem Lett 17: 819-22 (2007)
Procter & Gamble Pharmaceuticals
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Bioorg Med Chem Lett 17: 789-92 (2007)
Inserm U761 Biostructures And Drug Discovery Lille
MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus.
Bioorg Med Chem Lett 17: 832-5 (2007)
Procter & Gamble Pharmaceuticals
Evaluating scoring functions for docking and designing beta-secretase inhibitors.
Bioorg Med Chem Lett 17: 823-7 (2007)
Merck Research Laboratories
Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives.
Bioorg Med Chem Lett 17: 673-8 (2007)
Bayer Healthcare
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
Bioorg Med Chem Lett 17: 814-8 (2007)
Procter & Gamble Pharmaceuticals
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett 17: 363-9 (2007)
Argenta Discovery
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).
Bioorg Med Chem 15: 800-14 (2007)
Paradigm Pharmaceuticals
Discovery of Helicobacter pylori shikimate kinase inhibitors: bioassay and molecular modeling.
Bioorg Med Chem 15: 656-62 (2006)
Chinese Academy Of Sciences
Synthesis, nicotinic acetylcholine receptor binding, antinociceptive and seizure properties of methyllycaconitine analogs.
Bioorg Med Chem 15: 678-85 (2006)
Research Triangle Institute
Core exploration in optimization of chemokine receptor CCR4 antagonists.
Bioorg Med Chem Lett 17: 679-82 (2007)
Bristol-Myers Squibb Pharmaceutical Research Institute
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.
Bioorg Med Chem Lett 17: 732-5 (2007)
Glaxosmithkline
Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists.
Bioorg Med Chem Lett 17: 697-701 (2007)
Ucb Pharma
Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors.
Bioorg Med Chem Lett 17: 736-40 (2007)
Incyte
Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.
Bioorg Med Chem 15: 868-85 (2006)
Kissei Pharmaceutical
Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors.
Bioorg Med Chem 15: 727-34 (2006)
Central Drug Research Institute
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma.
Bioorg Med Chem Lett 17: 756-60 (2007)
Pfizer
Pharmacophore identification of KSP inhibitors.
Bioorg Med Chem Lett 17: 722-6 (2007)
China Pharmaceutical University
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.
Bioorg Med Chem Lett 17: 337-40 (2007)
Astrazeneca R&D Boston
Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
Bioorg Med Chem Lett 17: 745-9 (2007)
National Institute On Drug Abuse-Intramural Research Program
Evolution of thiazolidine-based blockers of human Kv1.5 for the treatment of atrial arrhythmias.
Bioorg Med Chem Lett 17: 282-4 (2006)
Procter And Gamble Pharmaceuticals
Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.
Bioorg Med Chem Lett 17: 354-7 (2007)
Paradigm Therapeutics
Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.
Bioorg Med Chem Lett 17: 533-7 (2007)
Institute For Degenerative Diseases
Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 17: 394-9 (2007)
Astrazeneca
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett 17: 370-5 (2007)
Argenta Discovery
Inhibition of metalloprotease botulinum serotype A from a pseudo-peptide binding mode to a small molecule that is active in primary neurons.
J Biol Chem 282: 5004-14 (2007)
National Cancer Institute-Frederick
Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.
Bioorg Med Chem Lett 17: 309-14 (2007)
Merck Research Laboratories
Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers.
Bioorg Med Chem Lett 17: 476-81 (2007)
Institute Of Science And Technology
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.
Bioorg Med Chem Lett 17: 828-31 (2007)
Merck Research Laboratories
Simple colorimetric inhibition assay of heme crystallization for high-throughput screening of antimalarial compounds.
Antimicrob Agents Chemother 51: 350-3 (2006)
Kyoto Institute Of Technology
Design, synthesis, and SAR analysis of novel selective sigma1 ligands.
Bioorg Med Chem 15: 771-83 (2006)
Università
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.
Bioorg Med Chem 15: 791-9 (2006)
Università
New competitive inhibitors of cytosolic (NADH-dependent) rabbit muscle glycerophosphate dehydrogenase.
Bioorg Med Chem Lett 17: 410-3 (2007)
Paris-Sud University
Simplified staurosporine analogs as potent JAK3 inhibitors.
Bioorg Med Chem Lett 17: 326-31 (2007)
Johnson & Johnson Pharmaceutical Research And Development
Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.
Bioorg Med Chem Lett 17: 807-13 (2007)
Merck Research Laboratories
Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety.
Bioorg Med Chem Lett 17: 761-6 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
Preparation of secolycorines against acetylcholinesterase.
Bioorg Med Chem 15: 1034-43 (2006)
National Taiwan University
Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.
Bioorg Med Chem 15: 886-96 (2007)
Universit£
Design and synthesis of rho kinase inhibitors (III).
Bioorg Med Chem 15: 1022-33 (2006)
Kirin Brewery
The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain.
Bioorg Med Chem Lett 17: 385-9 (2007)
Gsk
Studies towards the identification of a new generation of atypical antipsychotic agents.
Bioorg Med Chem Lett 17: 400-5 (2007)
Uk. Vinc
Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases.
Eur J Med Chem 42: 243-7 (2007)
Université
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.
Bioorg Chem 34: 424-44 (2006)
Medical College Of Wiscosin
CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives.
Bioorg Med Chem Lett 17: 231-4 (2006)
Berlex Biosciences
Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors.
Bioorg Med Chem 15: 1014-21 (2006)
Okayama University Graduate School Of Medicine
Novel nucleotide triphosphates as potent P2Y2 agonists with enhanced stability over UTP.
Bioorg Med Chem Lett 17: 558-61 (2007)
Ucb-Group
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.
Bioorg Med Chem Lett 17: 424-7 (2007)
Glaxosmithkline
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Bioorg Med Chem Lett 17: 511-6 (2007)
Schering-Plough Research Institute
Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound.
Antimicrob Agents Chemother 51: 119-27 (2007)
Microbiotix
Ring substituent effects on biological activity of vinyl sulfones as inhibitors of HIV-1.
Bioorg Med Chem 15: 1127-37 (2006)
University Of California
3D pharmacophore based virtual screening of T-type calcium channel blockers.
Bioorg Med Chem 15: 1091-105 (2006)
Institute Of Science And Technology
Novel poly(ADP-ribose) polymerase-1 inhibitors.
Bioorg Med Chem Lett 17: 542-5 (2007)
Cephalon
Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation.
Bioorg Med Chem Lett 17: 428-33 (2007)
Glaxosmithkline Medicine Research Centre
Deconstructing fragment-based inhibitor discovery.
Nat Chem Biol 2: 720-3 (2006)
TBA
Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors.
Bioorg Med Chem 15: 1044-55 (2006)
Astellas Pharm
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.
Bioorg Med Chem 15: 142-59 (2006)
Pfizer
A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.
Bioorg Med Chem 15: 63-76 (2006)
University Of Lille 2
Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters.
Bioorg Med Chem 15: 1067-82 (2006)
Organix
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
Bioorg Med Chem Lett 17: 40-4 (2006)
Abbott Laboratories
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
Bioorg Med Chem Lett 17: 491-4 (2007)
Universit£
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.
Bioorg Med Chem Lett 17: 527-32 (2007)
Abbott Laboratories
Synthesis and biological evaluation of methanesulfonamide analogues of rofecoxib: Replacement of methanesulfonyl by methanesulfonamido decreases cyclooxygenase-2 selectivity.
Bioorg Med Chem 15: 1056-61 (2006)
University Of Alberta Edmonton
Isolation, structure elucidation, and biological evaluation of 15-amido-3-demethoxy-2alpha,3alpha-methylenedioxyerythroculine, a new alkaloid from Hyperbaena valida.
J Nat Prod 69: 1514-6 (2006)
Glaxosmithkline
Indoleamine 2,3-dioxygenase inhibitors from the Northeastern Pacific Marine Hydroid Garveia annulata.
J Nat Prod 69: 1496-9 (2006)
University Of British Columbia
Microbial transformation and butyrylcholinesterase inhibitory activity of (-)-caryophyllene oxide and its derivatives.
J Nat Prod 69: 1429-34 (2006)
University Of Karachi
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
J Nat Prod 69: 1421-4 (2006)
Uppsala University
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.
Bioorg Med Chem 15: 174-85 (2006)
Chugai Pharmaceutical
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.
Bioorg Med Chem 15: 160-73 (2006)
Astellas Pharma
A Pd(0) based cross-coupling approach to the synthesis of 2-amidopurines and their evaluation as CDK inhibitors.
Bioorg Med Chem 15: 130-41 (2006)
Institut Curie
1-Methylpyridinium-4-(4-phenylmethanethiosulfonate) iodide, MTS-MPP+, a novel scanning cysteine accessibility method (SCAM) reagent for monoamine transporter studies.
Bioorg Med Chem 15: 305-11 (2007)
Purdue University
Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Bioorg Med Chem Lett 17: 486-90 (2007)
Pfizer
Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase.
Bioorg Med Chem Lett 17: 461-4 (2007)
Pusan National University
Synthesis and biological evaluation of novel T-type calcium channel blockers.
Bioorg Med Chem Lett 17: 471-5 (2007)
Kyung Hee University
Identification of potent and selective TACE inhibitors via the S1 pocket.
Bioorg Med Chem Lett 17: 34-9 (2006)
Wyeth Research
Design and synthesis of a novel photoaffinity ligand for the dopamine and serotonin transporters based on 2beta-carbomethoxy-3beta-biphenyltropane.
J Med Chem 49: 6621-5 (2006)
National Institute On Drug Abuse-Intramural Research Program
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
J Med Chem 49: 6607-13 (2006)
Università
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
J Med Chem 49: 6569-84 (2006)
Abbott Laboratories
Cyclic MrIA: a stable and potent cyclic conotoxin with a novel topological fold that targets the norepinephrine transporter.
J Med Chem 49: 6561-8 (2006)
University Of Queensland
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
J Med Chem 49: 6549-60 (2006)
Hoffmann-La Roche
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
J Med Chem 49: 6539-48 (2006)
Griffith University
Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3.
J Med Chem 49: 6532-8 (2006)
The Danish University Of Pharmaceutical Sciences
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
J Med Chem 49: 6500-9 (2006)
Palacky University
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
J Med Chem 49: 6465-88 (2006)
Astrazeneca
Further studies on imidazo[4,5-b]pyridine AT1 angiotensin II receptor antagonists. Effects of the transformation of the 4-phenylquinoline backbone into 4-phenylisoquinolinone or 1-phenylindene scaffolds.
J Med Chem 49: 6451-64 (2006)
Università
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
J Med Chem 49: 6439-42 (2006)
Abbott Laboratories
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
J Med Chem 49: 6435-8 (2006)
Pfizer
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.
Drug Metab Dispos 35: 150-67 (2006)
Bristol-Myers Squibb
Development of a novel dicistronic reporter-selectable hepatitis C virus replicon suitable for high-throughput inhibitor screening.
Antimicrob Agents Chemother 51: 95-102 (2006)
Pfizer
Identification of selective neuropeptide Y2 peptide agonists.
Bioorg Med Chem Lett 17: 538-41 (2007)
Bayer Pharmaceuticals
Intermediate analogue inhibitors of mandelate racemase: N-Hydroxyformanilide and cupferron.
Bioorg Med Chem Lett 17: 105-8 (2006)
Dalhousie University
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.
Bioorg Med Chem Lett 17: 501-6 (2007)
Covx Research
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Bioorg Med Chem Lett 17: 495-500 (2007)
Abbott Laboratories
Discovery of potent and selective PKC-theta inhibitors.
Bioorg Med Chem Lett 17: 225-30 (2006)
Boehringer Ingelheim Pharmaceuticals
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bioorg Med Chem Lett 17: 49-52 (2007)
Merck Research Laboratories
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.
Bioorg Med Chem Lett 17: 507-10 (2007)
Tufts University School Of Medicine
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 57-62 (2007)
Schering-Plough Research Institute
Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.
Bioorg Med Chem 15: 273-82 (2007)
University Of Cape Town
Synthesis of beta-ketophosphonate analogs of glutamyl and glutaminyl adenylate, and selective inhibition of the corresponding bacterial aminoacyl-tRNA synthetases.
Bioorg Med Chem 15: 295-304 (2007)
Crefsip
Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.
Bioorg Med Chem Lett 17: 118-22 (2006)
Wyeth Research
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.
Bioorg Med Chem 15: 403-12 (2007)
Astellas Pharma
Design of potent inhibitors of human beta-secretase. Part 2.
Bioorg Med Chem Lett 17: 78-81 (2006)
Pfizer
Design and synthesis of Rho kinase inhibitors (II).
Bioorg Med Chem 15: 350-64 (2006)
Kirin Brewery
Design of bioavailable derivatives of 12-(3-adamantan-1-yl-ureido)dodecanoic acid, a potent inhibitor of the soluble epoxide hydrolase.
Bioorg Med Chem 15: 312-23 (2006)
Department Of Entomology And University Of California Davis Cancer Center
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.
Bioorg Med Chem Lett 17: 205-7 (2007)
Schering-Plough Research Institute
Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety.
Bioorg Med Chem Lett 17: 132-5 (2006)
Universit£
Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase.
Bioorg Med Chem Lett 17: 136-41 (2006)
University College London
Design of potent inhibitors of human beta-secretase. Part 1.
Bioorg Med Chem Lett 17: 73-7 (2006)
Pfizer
N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists.
Bioorg Med Chem Lett 17: 161-6 (2006)
Cv Therapeutics
Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells.
Biopolymers 84: 595-604 (2006)
University Of California Davis
BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.
Biochem J 401: 29-38 (2007)
University Of Dundee
Tri-, tetra- and heptacyclic perylene analogues as new potential antineoplastic agents based on DNA telomerase inhibition.
Bioorg Med Chem 15: 555-62 (2006)
University Of Padova
Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Bioorg Med Chem 15: 365-73 (2006)
Institute Of Science And Technology
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
Bioorg Med Chem 15: 433-43 (2006)
National Institute Of Pharmaceutical Education And Research
Identification of novel, selective and potent Chk2 inhibitors.
Bioorg Med Chem Lett 17: 172-5 (2006)
Valeant Pharmaceutical Research And Development 3300 Hyland Avenue
2,6-Quinolinyl derivatives as potent VLA-4 antagonists.
Bioorg Med Chem Lett 17: 142-6 (2007)
Ucb Pharma
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.
Bioorg Med Chem Lett 17: 214-9 (2006)
Seoul National University
N-Substituted carbazolyloxyacetic acids modulate Alzheimer associated gamma-secretase.
Bioorg Med Chem Lett 17: 176-82 (2007)
Darmstadt University Of Technology
Identification of a series of highly potent activators of the Nurr1 signaling pathway.
Bioorg Med Chem Lett 17: 193-6 (2006)
Novartis Institutes For Biomedical Research
Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.
J Med Chem 49: 6421-4 (2006)
National Health Research Institutes
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
J Med Chem 49: 6416-20 (2006)
Abbott Laboratories
Dopamine/serotonin receptor ligands. 13: Homologization of a benzindoloazecine-type dopamine receptor antagonist modulates the affinities for dopamine D(1)-D(5) receptors.
J Med Chem 49: 6408-11 (2006)
Friedrich-Schiller-UniversitäT Jena
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
J Med Chem 49: 6391-9 (2006)
National Institute On Drug Abuse-Intramural Research Program
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.
J Med Chem 49: 6371-90 (2006)
Johnson And Johnson Pharmaceutical Research And Development
Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
J Med Chem 49: 6351-63 (2006)
Juvantia Pharma
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis.
J Med Chem 49: 6308-23 (2006)
University Of California San Francisco
Identification of selective, nonpeptidic nitrile inhibitors of cathepsin s using the substrate activity screening method.
J Med Chem 49: 6298-307 (2006)
University Of California Berkeley
Impact of species-dependent differences on screening, design, and development of MAO B inhibitors.
J Med Chem 49: 6264-72 (2006)
University Of Geneva
Conformationally restricted dipeptide amides as potent and selective neuronal nitric oxide synthase inhibitors.
J Med Chem 49: 6254-63 (2006)
Northwestern University
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.
J Med Chem 49: 6209-21 (2006)
University Of Newcastle Upon Tyne
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.
J Med Chem 49: 6170-6 (2006)
Neurocrine Biosciences
Synthesis and antiviral activity of 5-substituted cytidine analogues: identification of a potent inhibitor of viral RNA-dependent RNA polymerases.
J Med Chem 49: 6166-9 (2006)
The Pennsylvania State University
Acylguanidines as small-molecule beta-secretase inhibitors.
J Med Chem 49: 6158-61 (2006)
Wyeth Research
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.
J Med Chem 49: 6155-7 (2006)
Eli Lilly
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
J Med Chem 49: 6151-4 (2006)
Wyeth Research
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
J Med Chem 49: 6147-50 (2006)
Merck Research Laboratories
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
J Med Chem 49: 6143-6 (2006)
Ligand Pharmaceuticals
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
J Med Chem 49: 6139-42 (2006)
University Of Michigan
Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance.
Nat Chem Biol 2: 608-17 (2006)
University Of Cambridge
Probing cell-division phenotype space and Polo-like kinase function using small molecules.
Nat Chem Biol 2: 618-26 (2006)
Rockefeller University
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.
J Biol Chem 281: 38013-21 (2006)
Incyte
Synthesis, biological activity and molecular modelling of new trisubstituted 8-azaadenines with high affinity for A1 adenosine receptors.
Eur J Med Chem 42: 1-9 (2007)
Università
SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists.
Bioorg Med Chem Lett 17: 189-92 (2006)
Wyeth Research
Natural inhibitors targeting osteoclast-mediated bone resorption.
Bioorg Med Chem Lett 16: 6178-80 (2006)
Chinese Academy Of Sciences
Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies.
Bioorg Med Chem Lett 17: 272-7 (2006)
Ucb Pharma
Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.
Bioorg Med Chem Lett 17: 220-4 (2006)
Universit£
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
Bioorg Med Chem Lett 16: 6200-3 (2006)
Universit£
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bioorg Med Chem Lett 16: 6165-9 (2006)
Merck Research Laboratories
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett 17: 266-71 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.
Bioorg Med Chem Lett 17: 250-4 (2006)
Glaxosmithkline
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
J Pharmacol Exp Ther 320: 89-98 (2006)
Glaxosmithkline
In silico identification and biochemical characterization of novel inhibitors of NQO1.
Bioorg Med Chem Lett 16: 6246-54 (2006)
University Of Manchester
Novel nucleotide triphosphates as potent P2Y2 agonists.
Bioorg Med Chem Lett 17: 562-5 (2007)
Ucb-Group
Structural correlation between lipophilicity and lipopolysaccharide-sequestering activity in spermine-sulfonamide analogs.
Bioorg Med Chem Lett 16: 6209-12 (2006)
Mediquest Therapeutics
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 16: 6226-30 (2006)
Abbott Laboratories
Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers.
Bioorg Med Chem Lett 16: 6213-8 (2006)
Procter & Gamble Pharmaceuticals
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.
Bioorg Med Chem Lett 16: 6316-20 (2006)
Boehringer Ingelheim Pharmaceuticals
Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).
Bioorg Med Chem Lett 16: 5913-6 (2006)
Fudan University
Synthesis and evaluation of a small library of graftable thrombin inhibitors derived from (L)-arginine.
Eur J Med Chem 42: 37-53 (2007)
Université
Design, synthesis, biochemical evaluation and antimycobacterial action of phosphonate inhibitors of antigen 85C, a crucial enzyme involved in biosynthesis of the mycobacterial cell wall.
Eur J Med Chem 42: 54-63 (2007)
University Of Ljubljana
Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones.
Bioorg Med Chem 15: 575-85 (2006)
University Of Bologna
Structure-activity relationships of Bacillus cereus and Bacillus anthracis dihydrofolate reductase: toward the identification of new potent drug leads.
Antimicrob Agents Chemother 50: 3435-43 (2006)
University Of Connecticut At Storrs
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
Bioorg Med Chem Lett 16: 6328-33 (2006)
Eli Lilly
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
Bioorg Med Chem Lett 16: 6293-7 (2006)
Eli Lilly
Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.
J Med Chem 49: 6133-7 (2006)
Uppsala University
Curcumin and dehydrozingerone derivatives: synthesis, radiolabeling, and evaluation for beta-amyloid plaque imaging.
J Med Chem 49: 6111-9 (2006)
Sungkyunkwan University School Of Medicine
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
J Med Chem 49: 6104-10 (2006)
University Of Bristol
Evaluation of azasterols as anti-parasitics.
J Med Chem 49: 6094-103 (2006)
Cardiff University
Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor
J Med Chem 49: 6074-86 (2006)
Schering-Plough Research Institute
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
J Med Chem 49: 6046-56 (2006)
Sapienza University Of Rome
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
J Med Chem 49: 6037-45 (2006)
Universit£
Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol-3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase.
J Med Chem 49: 6027-36 (2006)
Wyeth
A novel class of potent nonglycosidic and nonpeptidic pan-selectin inhibitors.
J Med Chem 49: 5988-99 (2006)
Johannes Gutenberg University
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction.
J Med Chem 49: 5969-87 (2006)
University Of North Carolina At Greensboro
Antibacterial agent discovery using thymidylate synthase biolibrary screening.
J Med Chem 49: 5958-68 (2006)
Unimore
Design, synthesis, and biological evaluation of new 1,8-naphthyridin-4(1H)-on-3-carboxamide and quinolin-4(1H)-on-3-carboxamide derivatives as CB2 selective agonists.
J Med Chem 49: 5947-57 (2006)
Universit£
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
Bioorg Med Chem Lett 16: 6241-5 (2006)
Abbott Laboratories
Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.
Bioorg Med Chem Lett 16: 6281-7 (2006)
University Of Maryland
Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents.
Bioorg Med Chem Lett 16: 5978-81 (2006)
Merck Research Laboratories
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