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Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.
J Med Chem 47: 1575-86 (2004)
Pfizer
3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers.
J Med Chem 47: 1547-52 (2004)
Purdue Pharma
First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.
J Med Chem 47: 1536-46 (2004)
Uppsala University
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
J Med Chem 47: 1514-26 (2004)
University of Arizona
New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.
J Med Chem 47: 1475-86 (2004)
Harvard Medical School
Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents.
J Med Chem 47: 1448-64 (2004)
University of Caen Normandy
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
J Med Chem 47: 1434-47 (2004)
University of Ferrara
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
J Med Chem 47: 1400-12 (2004)
Southern Research Institute
Structure-based optimization of novel azepane derivatives as PKB inhibitors.
J Med Chem 47: 1375-90 (2004)
Roche Diagnostics
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
J Med Chem 47: 1351-9 (2004)
Sapienza University of Rome
Design and synthesis of new templates derived from pyrrolopyrimidine as selective multidrug-resistance-associated protein inhibitors in multidrug resistance.
J Med Chem 47: 1339-50 (2004)
Xenova
Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance.
J Med Chem 47: 1329-38 (2004)
Xenova
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.
J Med Chem 47: 1325-8 (2004)
Morphochem
Synthesis of a potent transition-state inhibitor of 5'-deoxy-5'-methylthioadenosine phosphorylase.
J Med Chem 47: 1322-4 (2004)
Biocryst Pharmaceuticals
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.
J Med Chem 47: 1319-21 (2004)
Glaxosmithkline
A non-peptide NK1 receptor agonist showing subpicomolar affinity.
J Med Chem 47: 1315-8 (2004)
Università
Selective optimization of side activities: another way for drug discovery.
J Med Chem 47: 1303-14 (2004)
Prestwick Chemical
Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.
Cancer Res 64: 1802-10 (2004)
The University of Birmingham
Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney.
Proc Natl Acad Sci U S A 101: 3569-74 (2004)
Tohoku University
FE200041 (D-Phe-D-Phe-D-Nle-D-Arg-NH2): A peripheral efficacious kappa opioid agonist with unprecedented selectivity.
J Pharmacol Exp Ther 310: 326-33 (2004)
University of Arizona
Biologically active compounds from Aphyllophorales (polypore) fungi.
J Nat Prod 67: 300-10 (2004)
The University of Mississippi
In vitro characterization of 5-carboxyl-2,4-di-benzamidobenzoic acid (NS3763), a noncompetitive antagonist of GLUK5 receptors.
J Pharmacol Exp Ther 309: 1003-10 (2004)
Neurosearch
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.
Nat Med 10: 262-7 (2004)
Vertex Pharmaceuticals
Design and synthesis of novel small molecule N/OFQ receptor antagonists.
Bioorg Med Chem Lett 14: 1347-51 (2004)
Purdue Pharma
A series of heterocyclic inhibitors of phenylalanyl-tRNA synthetases with antibacterial activity.
Bioorg Med Chem Lett 14: 1343-6 (2004)
Cubist Pharmaceuticals
A series of spirocyclic analogues as potent inhibitors of bacterial phenylalanyl-tRNA synthetases.
Bioorg Med Chem Lett 14: 1339-42 (2004)
Cubist Pharmaceuticals
Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine derivatives.
Bioorg Med Chem Lett 14: 1333-7 (2004)
Liaoning Normal University
Orally active PDE4 inhibitors with therapeutic potential.
Bioorg Med Chem Lett 14: 1323-7 (2004)
Minase Research Institute
Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!
Bioorg Med Chem Lett 14: 1317-21 (2004)
Merck Research Laboratories
Penicillin-derived inhibitors that simultaneously target both metallo- and serine-beta-lactamases.
Bioorg Med Chem Lett 14: 1299-304 (2004)
Southern Methodist University
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives: high-affinity ligands to the alpha 2 delta subunit of voltage gated calcium channels.
Bioorg Med Chem Lett 14: 1295-8 (2004)
Merck Research Laboratories
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.
Bioorg Med Chem Lett 14: 1291-4 (2004)
Schering-Plough Research Institute
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Bioorg Med Chem Lett 14: 1269-72 (2004)
Maxim Pharmaceuticals
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 1265-8 (2004)
Merck Research Laboratories
Novel non-peptidic neuropeptide Y Y2 receptor antagonists.
Bioorg Med Chem Lett 14: 1239-42 (2004)
Johnson & Johnson Pharmaceutical Research and Development
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Bioorg Med Chem Lett 14: 1229-34 (2004)
Millennium Pharmaceuticals
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.
Bioorg Med Chem Lett 14: 1221-7 (2004)
Millennium Pharmaceuticals
Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues.
Bioorg Med Chem Lett 14: 1213-6 (2004)
Pfizer
Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes.
Bioorg Med Chem Lett 14: 1205-7 (2004)
Nci-Frederick
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
Bioorg Med Chem Lett 14: 1201-3 (2004)
Merck Frosst Centre For Therapeutic Research
Design and synthesis of benzoxazole derivatives as novel melatoninergic ligands.
Bioorg Med Chem Lett 14: 1197-200 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel quinazoline-quinoline alkaloids with cytotoxic and DNA topoisomerase II inhibitory activities.
Bioorg Med Chem Lett 14: 1193-6 (2004)
Toho University
A novel class of apical sodium-dependent bile acid transporter inhibitors: the amphiphilic 4-oxo-1-phenyl-1,4-dihydroquinoline derivatives.
Bioorg Med Chem Lett 14: 1183-6 (2004)
Sankyo
Potent imidazole and triazole CB1 receptor antagonists related to SR141716.
Bioorg Med Chem Lett 14: 1151-4 (2004)
Neurocrine Biosciences
New heteroarylbenzenesulphonamides as matrix metalloproteinase inhibitors.
Bioorg Med Chem Lett 14: 1119-21 (2004)
Lille University of Science and Technology
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
J Pharmacol Sci 94: 197-202 (2004)
Kyorin University
S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.
J Pharmacol Exp Ther 309: 903-20 (2004)
Institut De Recherches Servier
Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.
J Med Chem 47: 1272-9 (2004)
Universita Degli Studi Di Firenze
Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.
J Med Chem 47: 1259-71 (2004)
Neurocrine Biosciences
Chemical and functional identification and characterization of novel sulfated alpha-conotoxins from the cone snail Conus anemone.
J Med Chem 47: 1234-41 (2004)
The University of Queensland
Synthesis of 2',5'-dideoxy-2-fluoroadenosine and 2',5'-dideoxy-2,5'-difluoroadenosine: potent P-site inhibitors of adenylyl cyclase.
J Med Chem 47: 1207-13 (2004)
National Institute of Diabetes and Digestive and Kidney Diseases
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
J Med Chem 47: 1193-206 (2004)
University of Colorado
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
J Med Chem 47: 1175-82 (2004)
Glaxosmithkline
Structure-activity studies of orexin a and orexin B at the human orexin 1 and orexin 2 receptors led to orexin 2 receptor selective and orexin 1 receptor preferring ligands.
J Med Chem 47: 1153-60 (2004)
University of Leipzig
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.
J Med Chem 47: 1122-35 (2004)
Emory University
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity.
J Med Chem 47: 1098-109 (2004)
Sapienza University of Rome
Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.
J Med Chem 47: 1085-97 (2004)
Abbott Laboratories
Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.
J Med Chem 47: 1081-4 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor.
J Med Chem 47: 1075-8 (2004)
Central Pharmaceutical Research Institute
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.
Structure 12: 215-26 (2004)
University of Dundee
Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.
J Biol Chem 279: 18727-32 (2004)
Vertex Pharmaceuticals
Importance of phenolic address groups in opioid kappa receptor selective antagonists.
J Med Chem 47: 1070-3 (2004)
Research Triangle Institute
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.
J Med Chem 47: 1060-9 (2004)
University of Tromsø
Inhibition of adenosine deaminase by novel 5:7 fused heterocycles containing the imidazo[4,5-e][1,2,4]triazepine ring system: a structure-activity relationship study.
J Med Chem 47: 1044-50 (2004)
University of Maryland
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
J Med Chem 47: 1031-43 (2004)
University of Bonn
Prediction of ligand binding affinity and orientation of xenoestrogens to the estrogen receptor by molecular dynamics simulations and the linear interaction energy method.
J Med Chem 47: 1018-30 (2004)
Vrije Universiteit Amsterdam
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators.
J Med Chem 47: 993-8 (2004)
University of Tennessee At Memphis
Synthesis, SAR, crystal structure, and biological evaluation of benzoquinoliziniums as activators of wild-type and mutant cystic fibrosis transmembrane conductance regulator channels.
J Med Chem 47: 962-72 (2004)
Université
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.
J Med Chem 47: 935-46 (2004)
University of Athens
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant.
J Med Chem 47: 928-34 (2004)
Sapienza University of Rome
Effects of C2-alkylation, N-alkylation, and N,N'-dialkylation on the stability and estrogen receptor interaction of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.
J Med Chem 47: 915-27 (2004)
Free University of Berlin
Conformer- and alignment-independent model for predicting structurally diverse competitive CYP2C9 inhibitors.
J Med Chem 47: 907-14 (2004)
Astrazeneca R&D
5-Fluorinated L-lysine analogues as selective induced nitric oxide synthase inhibitors.
J Med Chem 47: 900-6 (2004)
Pfizer
Recognition of privileged structures by G-protein coupled receptors.
J Med Chem 47: 888-99 (2004)
Novo Nordisk
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.
J Med Chem 47: 871-87 (2004)
Astrazeneca
A selective AT2 receptor ligand with a gamma-turn-like mimetic replacing the amino acid residues 4-5 of angiotensin II.
J Med Chem 47: 859-70 (2004)
Uppsala University
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
J Med Chem 47: 792-804 (2004)
Amorepacific R&D Center
Synthesis of a 5-methylindolyl-containing macrocycle that displays ultrapotent Grb2 SH2 domain-binding affinity.
J Med Chem 47: 788-91 (2004)
National Cancer Institute-Frederick
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.
J Med Chem 47: 769-87 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and SAR exploration of dinapsoline analogues.
Bioorg Med Chem 12: 715-34 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Imaging reversal of multidrug resistance in living mice with bioluminescence: MDR1 P-glycoprotein transports coelenterazine.
Proc Natl Acad Sci U S A 101: 1702-7 (2004)
Washington University
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.
Biol Psychiatry 55: 320-2 (2004)
Emory University
Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists.
Bioorg Med Chem Lett 14: 817-21 (2004)
F. Hoffmann-La Roche
3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists.
Bioorg Med Chem Lett 14: 813-6 (2004)
Glaxosmithkline
The design and synthesis of sulfonamides as caspase-1 inhibitors.
Bioorg Med Chem Lett 14: 809-12 (2004)
Pfizer
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Bioorg Med Chem Lett 14: 805-8 (2004)
Merck Frosst Canada
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.
Bioorg Med Chem Lett 14: 797-800 (2004)
Shire Biochem
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides.
Bioorg Med Chem Lett 14: 793-6 (2004)
Shire Biochem
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.
Bioorg Med Chem Lett 14: 787-91 (2004)
Seoul National University
Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent.
Bioorg Med Chem Lett 14: 783-6 (2004)
Bayer Research Center
Essential structural features of acetogenins: role of hydroxy groups adjacent to the bis-THF rings.
Bioorg Med Chem Lett 14: 779-82 (2004)
Kyoto University
Bile acid amides derived from chiral amino alcohols: novel antimicrobials and antifungals.
Bioorg Med Chem Lett 14: 773-7 (2004)
National Chemical Laboratory (Csir-Ncl)
Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.
Bioorg Med Chem Lett 14: 767-71 (2004)
Institut De Recherches Servier
Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).
Bioorg Med Chem Lett 14: 761-5 (2004)
Berlex Biosciences
Benzene-di-N-octylcarbamates as conformationally constrained phospholipase A(2) inhibitors.
Bioorg Med Chem Lett 14: 751-5 (2004)
National Chung-Hsing University
Fluorinated dihydroquinolines as potent n-NOS inhibitors.
Bioorg Med Chem Lett 14: 743-6 (2004)
Schering
Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives.
Bioorg Med Chem Lett 14: 739-42 (2004)
Boehringer Ingelheim (Canada)
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands.
Bioorg Med Chem Lett 14: 727-9 (2004)
Nps Pharmaceuticals
Design of small molecule ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 14: 719-22 (2004)
Glaxosmithkline
Inhibition of alpha-chymotrypsin with thiol-bearing substrate analogues in the presence of zinc ion.
Bioorg Med Chem Lett 14: 701-5 (2004)
Pohang University of Science and Technology
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.
Bioorg Med Chem Lett 14: 689-93 (2004)
Abbott Laboratories
Peptidyl aldehydes as slow-binding inhibitors of dual-specificity phosphatases.
Bioorg Med Chem Lett 14: 685-7 (2004)
The Ohio State University
2-hydroxy-4-isopropylbenzaldehyde, a potent partial tyrosinase inhibitor.
Bioorg Med Chem Lett 14: 681-3 (2004)
University of California
Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.
Bioorg Med Chem Lett 14: 677-80 (2004)
Merck Sharp & Dohme Research Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Bioorg Med Chem Lett 14: 673-6 (2004)
Abbott Laboratories
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.
Bioorg Med Chem Lett 14: 667-71 (2004)
Drexel University College of Medicine
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.
Bioorg Med Chem Lett 14: 657-61 (2004)
Nerviano
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Bioorg Med Chem Lett 14: 639-43 (2004)
Merck Research Laboratories
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.
Bioorg Med Chem Lett 14: 605-9 (2004)
Kingston University
Rational design and synthesis of selective BACE-1 inhibitors.
Bioorg Med Chem Lett 14: 601-4 (2004)
Merck Research Laboratories
Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y(5) antagonists.
Bioorg Med Chem Lett 14: 597-9 (2004)
Universidad De Navarra
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Bioorg Med Chem Lett 14: 591-6 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
Bioorg Med Chem Lett 14: 585-9 (2004)
Universidad De Santiago De Compostela
Inhibition kinetics of carba- and C-fucosyl analogues of GDP-fucose against fucosyltransferase V: implication for the reaction mechanism.
Bioorg Med Chem Lett 14: 571-3 (2004)
University of California Los Angeles
Plakolide A, a new gamma-lactone from the marine sponge Plakortis sp.
J Nat Prod 67: 110-1 (2004)
Harbor Branch Oceanographic Institution
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.
J Med Chem 47: 744-55 (2004)
Eli Lilly
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
J Med Chem 47: 735-43 (2004)
Biological Research Center of The Hungarian Academy of Sciences
4-[5-Fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]phenyl]-3,4,5,6- tetrahydro-2H-pyran-4-carboxamide, an orally active inhibitor of 5-lipoxygenase with improved pharmacokinetic and toxicology characteristics.
J Med Chem 47: 720-5 (2004)
Pfizer
Potent and selective conformationally restricted neuronal nitric oxide synthase inhibitors.
J Med Chem 47: 703-10 (2004)
Northwestern University
Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.
J Med Chem 47: 673-80 (2004)
National Center For Genetic Engineering and Biotechnology At Thailand
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.
J Med Chem 47: 663-72 (2004)
Leiden University
Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.
J Med Chem 47: 656-62 (2004)
Johnson and Johnson Pharmaceutical Research and Development
Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones.
J Med Chem 47: 644-55 (2004)
National Cancer Institute-Frederick
Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.
J Med Chem 47: 627-43 (2004)
Solvay Pharma
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.
J Med Chem 47: 612-26 (2004)
Globe Pharmaceutical R and Abbott Laboratories
Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding.
J Med Chem 47: 600-11 (2004)
University of Illinois
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.
J Med Chem 47: 588-99 (2004)
Glaxosmithkline
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
J Med Chem 47: 550-7 (2004)
University of Marburg
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
J Med Chem 47: 530-49 (2004)
Ucb Pharma
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
J Med Chem 47: 519-29 (2004)
Astrazeneca Pharmaceuticals
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.
J Med Chem 47: 497-508 (2004)
Florida A and M University
Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Naunyn Schmiedebergs Arch Pharmacol 369: 151-9 (2004)
UniversitÄT WÜRzburg
In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.
Eur J Pharmacol 483: 301-8 (2004)
University of Innsbruck
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.
J Pharmacol Exp Ther 309: 404-13 (2004)
Johnson & Johnson Pharmaceutical
Structural basis for dipeptide amide isoform-selective inhibition of neuronal nitric oxide synthase.
Nat Struct Mol Biol 11: 54-9 (2004)
University of California Irvine
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.
J Pharmacol Exp Ther 309: 348-55 (2004)
Wyeth Research
Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors.
J Med Chem 47: 467-74 (2004)
The Ohio State University
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.
J Med Chem 47: 456-66 (2004)
Eli Lilly
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
J Med Chem 47: 446-55 (2004)
University of Maryland
Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.
J Med Chem 47: 432-45 (2004)
Yale University
Synthesis and structure-activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase.
J Med Chem 47: 400-10 (2004)
Novo Nordisk
Application of CoMFA and CoMSIA 3D-QSAR and docking studies in optimization of mercaptobenzenesulfonamides as HIV-1 integrase inhibitors.
J Med Chem 47: 385-99 (2004)
University of Southern California
Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum.
J Med Chem 47: 345-54 (2004)
National Center For Genetic Engineering and Biotechnology At Thailand
Evaluation of P1'-diversified phosphinic peptides leads to the development of highly selective inhibitors of MMP-11.
J Med Chem 47: 325-36 (2004)
University of Athens
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
J Med Chem 47: 303-24 (2004)
Abbott Laboratories
Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.
J Med Chem 47: 296-302 (2004)
Research Triangle Institute
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
J Med Chem 47: 281-4 (2004)
Research Triangle Institute
Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist.
Eur J Pharmacol 483: 37-43 (2004)
Yamanouchi Pharmaceutical
A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization.
J Am Chem Soc 126: 34-5 (2004)
Fujisawa Pharmaceutical
Thermodynamics of the molecular and chiral recognition of cycloalkanols and camphor by modified beta-cyclodextrins possessing simple aromatic tethers.
J Org Chem 69: 173-80 (2004)
Nankai University
Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase.
Chem Biol 10: 1183-93 (2003)
UniversitÀ
New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties.
Bioorg Med Chem Lett 14: 549-52 (2003)
Cv Therapeutics
2-(Aminomethyl)-benzamide-based glycine transporter type-2 inhibitors.
Bioorg Med Chem Lett 14: 545-8 (2003)
Pharmacopeia
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).
Bioorg Med Chem Lett 14: 535-9 (2003)
Cv Therapeutics
7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.
Bioorg Med Chem Lett 14: 531-4 (2003)
Johnson & Johnson Pharmaceutical Research and Development
Binding of an imidazopyridoindole at imidazoline I2 receptors.
Bioorg Med Chem Lett 14: 527-9 (2003)
Virginia Commonwealth University
3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.
Bioorg Med Chem Lett 14: 523-6 (2003)
Virginia Commonwealth University
Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane.
Bioorg Med Chem Lett 14: 515-8 (2003)
Wyeth Research
Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.
Bioorg Med Chem Lett 14: 499-504 (2003)
Discovery Research-Dr. Reddy'S Laboratories
Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I2-imidazoline binding sites.
Bioorg Med Chem Lett 14: 491-3 (2003)
Instituto De QuíMica MéDica
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
Bioorg Med Chem Lett 14: 449-53 (2003)
The Scripps Research Institute
1,2-Diaryl-1-ethanone and pyrazolo [4,3-c] quinoline-4-one as novel selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 445-8 (2003)
Dr. Reddy'S Laboratories
Effects of fluorine substitution of cytosine analogues on the binding affinity to HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 14: 437-40 (2003)
The University of Georgia
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.
Bioorg Med Chem Lett 14: 413-6 (2004)
Technische Universitat Braunschweig
A novel series of potent and selective IKK2 inhibitors.
Bioorg Med Chem Lett 14: 409-12 (2003)
Celltech R&D
N-Benzylindole-2-carboxylic acids: potent functional antagonists of the CCR2b chemokine receptor.
Bioorg Med Chem Lett 14: 405-8 (2003)
Astrazeneca
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
Bioorg Med Chem Lett 14: 397-400 (2004)
Abbott Laboratories
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Bioorg Med Chem Lett 14: 383-7 (2003)
Pharmaceutical Research Institute
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.
Bioorg Med Chem Lett 14: 377-81 (2003)
Amgen
Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
Bioorg Med Chem Lett 14: 369-72 (2003)
University of Paris
A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors.
Bioorg Med Chem Lett 14: 357-60 (2003)
Novartis Institute For Biomedical Research
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Bioorg Med Chem Lett 14: 351-5 (2004)
Merck Research Laboratories
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.
Bioorg Med Chem Lett 14: 343-6 (2004)
Bristol-Myers Squibb
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
Bioorg Med Chem Lett 14: 337-41 (2003)
Bruker-Axs
Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors.
Bioorg Med Chem Lett 14: 333-6 (2003)
Taisho Pharmaceutical
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.
Bioorg Med Chem Lett 14: 325-8 (2003)
Ribotargets
Parallel solid-phase synthesis of disubstituted (5-biphenyltetrazolyl) hydantoins and thiohydantoins targeting the growth hormone secretagogue receptor.
Bioorg Med Chem Lett 14: 317-20 (2003)
Novo Nordisk
4,5-Disubstituted-1,3-oxazolidin-2-imine derivatives: a new class of orally bioavailable nitric oxide synthase inhibitor.
Bioorg Med Chem Lett 14: 313-6 (2003)
Dainippon Pharmaceutical
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.
Bioorg Med Chem Lett 14: 309-12 (2003)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
J Med Chem 47: 262-72 (2003)
Universita Degli Studi Di Firenze
Cyclodextrin-derived diorganyl tellurides as glutathione peroxidase mimics and inhibitors of thioredoxin reductase and cancer cell growth.
J Med Chem 47: 233-9 (2004)
Uppsala University
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.
J Med Chem 47: 196-209 (2003)
Johnson and Johnson Pharmaceutical Research and Development
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.
J Med Chem 47: 175-87 (2003)
University of Illinois At Urbana-Champaign
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
J Med Chem 47: 165-74 (2003)
Harvard Medical School
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.
J Med Chem 47: 158-64 (2004)
Elan Pharmaceuticals
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
J Med Chem 47: 143-57 (2003)
University of Siena
NMR structural characterization of peptide inhibitors bound to the Hepatitis C virus NS3 protease: design of a new P2 substituent.
J Med Chem 47: 123-32 (2003)
Boehringer Ingelheim (Canada)
Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity.
J Med Chem 47: 110-22 (2004)
Uppsala University
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.
J Med Chem 47: 101-9 (2003)
Central Pharmaceutical Research Institute
Design, synthesis, molecular modeling studies, and calpain inhibitory activity of novel alpha-ketoamides incorporating polar residues at the P1'-position.
J Med Chem 47: 72-9 (2003)
University of Tennessee Health Science Center
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.
J Med Chem 47: 37-44 (2004)
University of Queensland
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.
J Med Chem 47: 22-36 (2004)
Universitat Hamburg
Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase.
J Med Chem 47: 18-21 (2003)
Boehringer Ingelheim (Canada)
Discovery of alpha,gamma-diketo acids as potent selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase.
J Med Chem 47: 14-7 (2003)
Italy. Vinc
Self-association of okadaic acid upon complexation with potassium ion.
J Med Chem 47: 10-3 (2003)
Instituto Universitario De Bio-Organica Antonio Gonzalez
Isolation and structure elucidation of Sch 642305, a novel bacterial DNA primase inhibitor produced by Penicillium verrucosum.
J Nat Prod 66: 1527-30 (2003)
Schering-Plough Research Institute
Secondary mutations M36I and A71V in the human immunodeficiency virus type 1 protease can provide an advantage for the emergence of the primary mutation D30N.
Biochemistry 42: 15029-35 (2003)
University of Florida College of Medicine
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
Bioorg Med Chem Lett 14: 283-7 (2003)
Methylgene
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
Bioorg Med Chem Lett 14: 275-8 (2003)
Glaxosmithkline
Synthesis and nicotinic receptor activity of a hydroxylated tropane.
Bioorg Med Chem Lett 14: 271-3 (2003)
University of Wollongong
Structure-activity relationships of novel potent MurF inhibitors.
Bioorg Med Chem Lett 14: 267-70 (2003)
Abbott Laboratories
Novel P4 truncated tripeptidyl alpha-ketoamides as HCV protease inhibitors.
Bioorg Med Chem Lett 14: 263-6 (2003)
Eli Lilly
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.
Bioorg Med Chem Lett 14: 257-61 (2003)
Eli Lilly
Discovery of a novel bicycloproline P2 bearing peptidyl alpha-ketoamide LY514962 as HCV protease inhibitor.
Bioorg Med Chem Lett 14: 251-6 (2003)
Eli Lilly
P3 cap modified Phe*-Ala series BACE inhibitors.
Bioorg Med Chem Lett 14: 245-50 (2003)
Eli Lilly
Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.
Bioorg Med Chem Lett 14: 239-43 (2003)
Eli Lilly
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase.
Bioorg Med Chem Lett 14: 231-4 (2003)
Universita Degli Studi Di Firenze
Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits.
Bioorg Med Chem Lett 14: 225-9 (2003)
University of Montpellier
Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX.
Bioorg Med Chem Lett 14: 217-23 (2003)
Universita Degli Studi Di Firenze
Novel targeting strategy based on multimeric ligands for drug delivery and molecular imaging: homooligomers of alpha-MSH.
Bioorg Med Chem Lett 14: 211-5 (2003)
University of Arizona
Highly potent PDE4 inhibitors with therapeutic potential.
Bioorg Med Chem Lett 14: 207-10 (2004)
Minase Research Institute
Inactivation of gamma-aminobutyric acid aminotransferase by (S)-4-amino-4,5-dihydro-2-furancarboxylic acid does not proceed by the expected aromatization mechanism.
Bioorg Med Chem Lett 14: 203-6 (2003)
Northwestern University
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
Bioorg Med Chem Lett 14: 195-202 (2003)
Wake Forest University School of Medicine
Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.
Bioorg Med Chem Lett 14: 187-90 (2003)
Sugen
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
Bioorg Med Chem Lett 14: 181-5 (2003)
Sri International
Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1.
Bioorg Med Chem Lett 14: 177-80 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists.
Bioorg Med Chem Lett 14: 167-70 (2003)
Eli Lilly
The difluoromethylene group as a replacement for the labile oxygen in steroid sulfates: a new approach to steroid sulfatase inhibitors.
Bioorg Med Chem Lett 14: 151-5 (2003)
University of Waterloo
An electrochemical device for the assay of the interaction between a dioxin receptor and its various ligands.
Bioorg Med Chem Lett 14: 137-41 (2003)
Kyushu University
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.
Bioorg Med Chem Lett 14: 119-24 (2003)
Boehringer Ingelheim (Canada)
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
Bioorg Med Chem Lett 14: 111-4 (2004)
Glaxosmithkline
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Bioorg Med Chem Lett 14: 95-8 (2003)
Pfizer
Investigation of novel fumagillin analogues as angiogenesis inhibitors.
Bioorg Med Chem Lett 14: 91-4 (2003)
Gilead Sciences
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.
Bioorg Med Chem Lett 14: 87-90 (2003)
Amgen
The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
Bioorg Med Chem Lett 14: 81-5 (2003)
Inotek Pharmaceuticals
Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors.
Bioorg Med Chem Lett 14: 77-9 (2003)
The Ohio State University
Novel O-glycosyl amino acid mimetics as building blocks for O-glycopeptides act as inhibitors of galactosidases.
Bioorg Med Chem Lett 14: 73-5 (2003)
University of Hamburg
A facile synthesis of 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, a selective 15-lipoxygenase inhibitor.
Bioorg Med Chem Lett 14: 63-5 (2003)
Tamkang University
Peptide deformylase inhibitors with activity against respiratory tract pathogens.
Bioorg Med Chem Lett 14: 59-62 (2003)
British Biotech Pharmaceuticals
Discovery of a novel series of DHODH inhibitors by a docking procedure and QSAR refinement.
Bioorg Med Chem Lett 14: 55-8 (2003)
4Sc
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.
Bioorg Med Chem Lett 14: 47-50 (2003)
Chinese Academy of Sciences
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 43-6 (2003)
Merck
Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors.
Bioorg Med Chem Lett 14: 37-41 (2003)
Wyeth Research
New orally active PDE4 inhibitors with therapeutic potential.
Bioorg Med Chem Lett 14: 29-32 (2004)
Minase Research Institute
Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity.
Bioorg Med Chem Lett 14: 21-4 (2003)
Pfizer
Characterization of uremic toxin transport by organic anion transporters in the kidney.
Kidney Int 65: 162-74 (2004)
University of Tokyo
2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
J Med Chem 46: 5834-43 (2003)
The Danish University of Pharmaceutical Sciences
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
J Med Chem 46: 5812-24 (2003)
Vrije Universiteit Amsterdam
Generation of bis-cationic heterocyclic inhibitors of Bacillus subtilis HPr kinase/phosphatase from a ditopic dynamic combinatorial library.
J Med Chem 46: 5803-11 (2003)
Isis-Universit£
Novel lavendamycin analogues as potent HIV-reverse transcriptase inhibitors: synthesis and evaluation of anti-reverse transcriptase activity of amide and ester analogues of lavendamycin.
J Med Chem 46: 5773-80 (2003)
Ball State University
Synthesis and structure-activity relationship of mannose-based peptidomimetics selectively blocking integrin alpha4beta7 binding to mucosal addressin cell adhesion molecule-1.
J Med Chem 46: 5752-62 (2003)
Technische UniversitäT MüNchen
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
J Med Chem 46: 5745-51 (2003)
In2Gen
Parallel solid-phase synthesis and evaluation of inhibitors of Streptomyces coelicolor type II dehydroquinase.
J Med Chem 46: 5735-44 (2003)
Universidad De Santiago De Compostela
Three-dimensional quantitative structure-activity relationship analyses of peptide substrates of the mammalian H+/peptide cotransporter PEPT1.
J Med Chem 46: 5725-34 (2003)
Martin-Luther-University Halle-Wittenberg
Computer modeling of selective regions in the active site of nitric oxide synthases: implication for the design of isoform-selective inhibitors.
J Med Chem 46: 5700-11 (2003)
Northwestern University
Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations.
J Med Chem 46: 5691-9 (2003)
Yale University
Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors.
J Med Chem 46: 5663-73 (2003)
Quorex Pharmaceuticals
Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.
J Med Chem 46: 5651-62 (2003)
Leo Pharma
Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives.
J Med Chem 46: 5638-50 (2003)
Universidad Complutense
Rational design of an indolebutanoic acid derivative as a novel aldose reductase inhibitor based on docking and 3D QSAR studies of phenethylamine derivatives.
J Med Chem 46: 5619-27 (2003)
Yonsei University
Novel sst(4)-selective somatostatin (SRIF) agonists. 4. Three-dimensional consensus structure by NMR.
J Med Chem 46: 5606-18 (2003)
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
J Med Chem 46: 5597-605 (2003)
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
J Med Chem 46: 5587-96 (2003)
Salk Institute
Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
J Med Chem 46: 5579-86 (2003)
Salk Institute
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.
J Med Chem 46: 5567-70 (2003)
University of Wisconsin-Milwaukee
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist.
Eur J Pharmacol 482: 335-7 (2003)
Virginia Commonwealth University
Ligand structure-activity requirements and phospholipid dependence for the binding of phorbol esters to protein kinase D.
Mol Pharmacol 64: 1342-8 (2003)
University of Pittsburgh
Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling.
Mol Pharmacol 64: 1295-308 (2003)
Glaxosmithkline
Characterization of human alpha 4 beta 2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cells.
Mol Pharmacol 64: 1283-94 (2003)
Barrow Neurological Institute
Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione.
Int J Biochem Cell Biol 36: 247-57 (2004)
National University of Singapore
Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
Bioorg Med Chem Lett 13: 4505-9 (2003)
University of Florida
Structure-activity relationships of indole cytosolic phospholipase A(2)alpha inhibitors: substrate mimetics.
Bioorg Med Chem Lett 13: 4501-4 (2003)
Wyeth Research
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.
Bioorg Med Chem Lett 13: 4497-9 (2003)
Banyu Tsukuba Research Institute
Novel mechanism of inhibiting beta-lactamases by sulfonylation using beta-sultams.
Bioorg Med Chem Lett 13: 4489-92 (2003)
The University of Huddersfield
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake.
Bioorg Med Chem Lett 13: 4477-80 (2003)
Eli Lilly
Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2.
Bioorg Med Chem Lett 13: 4467-71 (2003)
Johnson & Johnson Pharmaceutical Research & Development
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Bioorg Med Chem Lett 13: 4459-62 (2003)
Adolor
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype.
Bioorg Med Chem Lett 13: 4431-5 (2003)
Merck Research Laboratories
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Bioorg Med Chem Lett 13: 4421-5 (2003)
Virginia Commonwealth University
Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs.
Bioorg Med Chem Lett 13: 4415-9 (2003)
Centre De Recherche De Paris
Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.
Bioorg Med Chem Lett 13: 4409-13 (2003)
Nps Pharmaceuticals
Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity.
Bioorg Med Chem Lett 13: 4405-8 (2003)
Università
Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects.
Bioorg Med Chem Lett 13: 4389-93 (2003)
Seoul National University
Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.
Bioorg Med Chem Lett 13: 4385-8 (2003)
Merck Research Laboratories
Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.
Bioorg Med Chem Lett 13: 4381-4 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
3D-QSAR studies on natural acetylcholinesterase inhibitors of Sarcococca saligna by comparative molecular field analysis (CoMFA).
Bioorg Med Chem Lett 13: 4375-80 (2003)
University of Innsbruck
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Bioorg Med Chem Lett 13: 4365-9 (2003)
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&Jprd)
4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.
Bioorg Med Chem Lett 13: 4361-4 (2003)
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&Jprd)
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI).
Bioorg Med Chem Lett 13: 4355-9 (2003)
Biogen
beta-alanine dipeptides as MC4R agonists.
Bioorg Med Chem Lett 13: 4341-4 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of statine-containing BACE inhibitors.
Bioorg Med Chem Lett 13: 4335-9 (2003)
Eli Lilly
Catechol-substituted L-chicoric acid analogues as HIV integrase inhibitors.
Bioorg Med Chem Lett 13: 4331-4 (2003)
Institute of Science & Technology
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.
Bioorg Med Chem Lett 13: 4321-6 (2003)
Nagoya City University
6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase.
Bioorg Med Chem Lett 13: 4313-6 (2003)
Novartis Forschungsinstitut
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Bioorg Med Chem Lett 13: 4299-304 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Bioorg Med Chem Lett 13: 4293-7 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Lysine sulfonamides as novel HIV-protease inhibitors: optimization of the Nepsilon-acyl-phenyl spacer.
Bioorg Med Chem Lett 13: 4289-92 (2003)
Pharmacor
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.
Bioorg Med Chem Lett 13: 4285-8 (2003)
Merck Research Laboratories
B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens.
Bioorg Med Chem Lett 13: 4281-4 (2003)
Eli Lilly
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
Bioorg Med Chem Lett 13: 4277-9 (2003)
Fujisawa Pharmaceutical
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.
Bioorg Med Chem Lett 13: 4273-6 (2003)
Kyoto Pharmaceutical University
Muscarinic mechanisms of antipsychotic atypicality.
Prog Neuropsychopharmacol Biol Psychiatry 27: 1125-43 (2003)
Eli Lilly
Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a novel tumor targeting concept.
J Med Chem 46: 5546-51 (2003)
Mcgill University Health Center/Royal Victoria Hospital
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
J Med Chem 46: 5512-32 (2003)
Faes Farma
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
J Med Chem 46: 5505-11 (2003)
University of Bath
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
J Med Chem 46: 5484-504 (2003)
Nitromed
Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates.
J Med Chem 46: 5471-7 (2003)
University of Montpellier
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
J Med Chem 46: 5445-57 (2003)
Vrije Universiteit
Pyrazole and isoxazole derivatives as new, potent, and selective 20-hydroxy-5,8,11,14-eicosatetraenoic acid synthase inhibitors.
J Med Chem 46: 5416-27 (2003)
Taisho Pharmaceutical
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin
J Med Chem 46: 5375-88 (2003)
Cephalon
Characterization of the 5-HT(7) receptor. Determination of the pharmacophore for 5-HT(7) receptor agonism and CoMFA-based modeling of the agonist binding site.
J Med Chem 46: 5365-74 (2003)
State University of Groningen
Application of the lambda-dynamics method to evaluate the relative binding free energies of inhibitors to HCV protease.
J Med Chem 46: 5360-4 (2003)
Schering-Plough Research Institute
Molecular model of the alpha(IIb)beta(3) integrin.
J Med Chem 46: 5316-25 (2003)
Merck Research Laboratories
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
J Med Chem 46: 5298-315 (2003)
Pharmaceutical Research Institute
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
J Med Chem 46: 5294-7 (2003)
Merck Research Laboratories
Design, synthesis, and biological activity of a difluoro-substituted, conformationally rigid vigabatrin analogue as a potent gamma-aminobutyric acid aminotransferase inhibitor.
J Med Chem 46: 5292-3 (2003)
Northwestern University
A new acylated oleanane triterpenoid from Couepia polyandra that inhibits the lyase activity of DNA polymerase beta.
J Nat Prod 66: 1463-5 (2003)
Virginia Polytechnic Institute and State University
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.
Cancer Res 63: 7861-9 (2003)
Abbott Laboratories
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
Bioorg Med Chem Lett 13: 4229-33 (2003)
Morphochem
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
Bioorg Med Chem Lett 13: 4217-21 (2003)
Gsk
Novel oxazolidinone-quinolone hybrid antimicrobials.
Bioorg Med Chem Lett 13: 4213-6 (2003)
Vicuron Pharmaceuticals
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 2: achieving activity in vivo through the use of alternative scaffolds.
Bioorg Med Chem Lett 13: 4205-8 (2003)
Daiichi Pharmaceutical
Semi-synthetic glycopeptide antibacterials.
Bioorg Med Chem Lett 13: 4165-8 (2003)
Theravance
Multidrug resistance to HIV-1 protease inhibition requires cooperative coupling between distal mutations.
Biochemistry 42: 13659-66 (2003)
The Johns Hopkins University
Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase.
J Med Chem 46: 5271-6 (2003)
Industrial Research
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.
J Med Chem 46: 5258-70 (2003)
University of Colorado
5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.
J Med Chem 46: 5249-57 (2003)
Abbott Laboratories
Synthesis, activity, and molecular modeling studies of novel human aldose reductase inhibitors based on a marine natural product.
J Med Chem 46: 5208-21 (2003)
Instituto Biomar
Dimerization inhibitors of HIV-1 protease based on a bicyclic guanidinium subunit.
J Med Chem 46: 5196-207 (2003)
Universidad Aut£Noma De Madrid
Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J Med Chem 46: 5184-95 (2003)
Aventis Pharma
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.
J Med Chem 46: 5171-83 (2003)
University of Illinois At Urbana-Champaign
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
J Med Chem 46: 5162-70 (2003)
Harvard Medical School
An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region.
J Med Chem 46: 5139-52 (2003)
Forbes Norris Als/Mda Research Center
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
J Med Chem 46: 5121-4 (2003)
Eli Lilly
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
J Med Chem 46: 5117-20 (2003)
Glaxosmithkline R&D
Rapid diversity-oriented synthesis in microtiter plates for in situ screening of HIV protease inhibitors.
Chembiochem 4: 1246-8 (2003)
The Scripps Research Institute
Two antiviral compounds from the plant Stylogne cauliflora as inhibitors of HCV NS3 protease.
Bioorg Med Chem Lett 13: 2925-8 (2003)
Schering-Plough Research Institute
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
Bioorg Med Chem Lett 13: 2921-4 (2003)
Neurogen
Microcystin analogues comprised only of Adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors.
Bioorg Med Chem Lett 13: 2907-11 (2003)
University of California Irvine
Linearized and truncated microcystin analogues as inhibitors of protein phosphatases 1 and 2A.
Bioorg Med Chem Lett 13: 2903-6 (2003)
University of California Irvine
Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity.
Bioorg Med Chem Lett 13: 2895-8 (2003)
Roche Research Center
Antitumor agents. Part 226: synthesis and cytotoxicity of 2-phenyl-4-quinolone acetic acids and their esters.
Bioorg Med Chem Lett 13: 2891-3 (2003)
University of North Carolina
Cage amines as the stopper inhibitors of cholinesterases.
Bioorg Med Chem Lett 13: 2887-90 (2003)
National Chung-Hsing University
Differentially functionalized diamines as novel ligands for the NPY2 receptor.
Bioorg Med Chem Lett 13: 2883-5 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.
Bioorg Med Chem Lett 13: 2875-8 (2003)
University of Antwerp
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
Bioorg Med Chem Lett 13: 2867-73 (2003)
University of Florence
MMPs inhibitors: new succinylhydroxamates with selective inhibition of MMP-2 over MMP-3.
Bioorg Med Chem Lett 13: 2843-6 (2003)
Umr/Cnrs 6013
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.
Bioorg Med Chem Lett 13: 2833-6 (2003)
Sankyo
Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.
Bioorg Med Chem Lett 13: 2829-32 (2003)
Sankyo
Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity.
Bioorg Med Chem Lett 13: 2825-8 (2003)
University of Bristol
Pharmacological and genetic characterization of two selective serotonin transporter ligands: 2-[2-(dimethylaminomethylphenylthio)]-5-fluoromethylphenylamine (AFM) and 3-amino-4-[2-(dimethylaminomethyl-phenylthio)]benzonitrile (DASB).
J Pharmacol Exp Ther 308: 481-6 (2004)
National Institutes of Health
Synthesis of a diverse library of mechanism-based cysteine protease inhibitors.
J Comb Chem 5: 869-80 (2003)
University of California Berkeley
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.
Science 302: 875-878 (2003)
Pfizer
High affinity, bioavailable 3-amino-1,4-benzodiazepine-based gamma-secretase inhibitors.
Bioorg Med Chem Lett 13: 4143-5 (2003)
Merck Sharp & Dohme Research Laboratories
Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes.
Bioorg Med Chem Lett 13: 4133-7 (2003)
Organix
A new class of glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 13: 4125-8 (2003)
Merck Research Laboratories
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Bioorg Med Chem Lett 13: 4121-4 (2003)
Novartis Institute of Biomedical Research
Inhibitory effects on mitochondrial complex I of semisynthetic mono-tetrahydrofuran acetogenin derivatives.
Bioorg Med Chem Lett 13: 4101-5 (2003)
Universidad De Valencia
Utility of boron clusters for drug design. Relation between estrogen receptor binding affinity and hydrophobicity of phenols bearing various types of carboranyl groups.
Bioorg Med Chem Lett 13: 4089-92 (2003)
Tohoku Pharmaceutical University
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.
Bioorg Med Chem Lett 13: 4085-8 (2003)
Toa Eiyo
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Bioorg Med Chem Lett 13: 4071-5 (2003)
Ligand Pharmaceuticals
Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants.
Bioorg Med Chem Lett 13: 4059-63 (2003)
Vertex Pharmaceuticals
Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.
Bioorg Med Chem Lett 13: 4047-50 (2003)
Astrazeneca R&D Charnwood
Novel P2X7 receptor antagonists.
Bioorg Med Chem Lett 13: 4043-6 (2003)
Astrazeneca
2,5-disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists.
Bioorg Med Chem Lett 13: 4031-4 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.
Bioorg Med Chem Lett 13: 4027-30 (2003)
Merck Research Laboratories
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.
Bioorg Med Chem Lett 13: 4015-7 (2003)
Yale University
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).
Bioorg Med Chem Lett 13: 4007-10 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Bioorg Med Chem Lett 13: 4001-5 (2003)
Abbott Laboratories
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.
Bioorg Med Chem Lett 13: 3997-4000 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Bioorg Med Chem Lett 13: 3983-7 (2003)
Merck Research Laboratories
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.
Bioorg Med Chem Lett 13: 3979-82 (2003)
Merck Research Laboratories
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.
Bioorg Med Chem Lett 13: 3975-8 (2003)
Memorial Sloan-Kettering Cancer Center
Synthesis of 2-fluoronoraristeromycin and its inhibitory activity against Plasmodium falciparum S-adenosyl-L-homocysteine hydrolase.
Bioorg Med Chem Lett 13: 3963-5 (2003)
Gifu University
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
Bioorg Med Chem Lett 13: 3947-50 (2003)
Abbott Laboratories
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3.
Bioorg Med Chem Lett 13: 3939-42 (2003)
Eli Lilly
Heterocyclic ketones as inhibitors of histone deacetylase.
Bioorg Med Chem Lett 13: 3909-13 (2003)
Abbott Laboratories
Green tea catechins as a BACE1 (beta-secretase) inhibitor.
Bioorg Med Chem Lett 13: 3905-8 (2003)
Kyungpook National University
Human organic anion transporter 3 (hOAT3) can operate as an exchanger and mediate secretory urate flux.
Cell Physiol Biochem 13: 249-56 (2003)
Georg-August-Universit£T
Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.
J Med Chem 46: 5091-4 (2003)
Novartis Research Institute Vienna
Molecular docking studies of natural cholinesterase-inhibiting steroidal alkaloids from Sarcococca saligna.
J Med Chem 46: 5087-90 (2003)
University of Innsbruck
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.
J Med Chem 46: 5074-82 (2003)
Duquesne University
Synthesis and biological evaluation of 5-substituted derivatives of the potent antiherpes agent (north)-methanocarbathymine.
J Med Chem 46: 5045-54 (2003)
National Cancer Institute-Frederick
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.
J Med Chem 46: 5005-14 (2003)
University of Antwerp (Uia)
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
J Med Chem 46: 4974-87 (2003)
Niddk
Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.
J Med Chem 46: 4965-73 (2003)
University of Arizona
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.
J Med Chem 46: 4952-64 (2003)
Glaxosmithkline Pharmaceuticals
Synthesis, characterization, and biological properties of 8-azido- and 8-amino-substituted 2',5'-oligoadenylates.
J Med Chem 46: 4926-32 (2003)
Gunma University
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
J Med Chem 46: 4910-25 (2003)
Pharmaceutical Research Institute
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.
J Med Chem 46: 4895-903 (2003)
University of Bologna
Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
J Med Chem 46: 4883-94 (2003)
Novo Nordisk
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
J Med Chem 46: 4872-82 (2003)
University of Alberta
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
J Med Chem 46: 4847-59 (2003)
Niddk
Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
J Med Chem 46: 4834-7 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
J Med Chem 46: 4826-9 (2003)
Sapienza University of Rome
Semiplenamides A-G, fatty acid amides from a Papua New Guinea collection of the marine cyanobacterium Lyngbya semiplena.
J Nat Prod 66: 1364-8 (2003)
Oregon State University
Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.
J Nat Prod 66: 1338-44 (2003)
Merck Research Laboratories
Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats.
Neuropharmacology 45: 935-44 (2003)
Eli Lilly
Selective COX-2 inhibition and cardiovascular effects: a review of the rofecoxib development program.
Am Heart J 146: 591-604 (2003)
University of Maryland Hospital
Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.
J Med Chem 46: 4799-802 (2003)
Wayne State University School of Medicine
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
J Med Chem 46: 4790-8 (2003)
Merck Research Laboratories
Potent inhibition of NTPase/helicase of the West Nile Virus by ring-expanded ("fat") nucleoside analogues.
J Med Chem 46: 4776-89 (2003)
University of Maryland
Finding discriminating structural features by reassembling common building blocks.
J Med Chem 46: 4770-5 (2003)
Leadscope
Adenosine kinase inhibitors. 3. Synthesis, SAR, and antiinflammatory activity of a series of l-lyxofuranosyl nucleosides.
J Med Chem 46: 4750-60 (2003)
Metabasis Therapeutics
Azasterols as inhibitors of sterol 24-methyltransferase in Leishmania species and Trypanosoma cruzi.
J Med Chem 46: 4714-27 (2003)
Cardiff University
Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase.
J Med Chem 46: 4702-13 (2003)
Roche Palo Alto
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.
J Med Chem 46: 4696-701 (2003)
Pharmacia
Molecular determinants of steroid inhibition for the mouse constitutive androstane receptor.
J Med Chem 46: 4687-95 (2003)
University of Kuopio
Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
J Med Chem 46: 4676-86 (2003)
Boehringer Ingelheim Pharmaceuticals
Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.
J Med Chem 46: 4669-75 (2003)
Boehringer Ingelheim Pharmaceuticals
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.
J Med Chem 46: 4657-68 (2003)
University of Tennessee Health Sciences Center
Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3 beta) from a library of compound searching.
J Med Chem 46: 4631-3 (2003)
Instituto De Quimica Medica (Csic)
Human beta-secretase (BACE) and BACE inhibitors.
J Med Chem 46: 4625-30 (2003)
Elan Pharmaceuticals
Sulphonamide-based small molecule VLA-4 antagonists.
Bioorg Med Chem Lett 13: 3875-8 (2003)
Molecumetics
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Bioorg Med Chem Lett 13: 3859-61 (2003)
Gedeon Richter
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.
Bioorg Med Chem Lett 13: 3841-6 (2003)
Eli Lilly
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.
Bioorg Med Chem Lett 13: 3835-9 (2003)
Eli Lilly
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
Bioorg Med Chem Lett 13: 3821-5 (2003)
Abbott Laboratories
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
Bioorg Med Chem Lett 13: 3817-20 (2003)
Abbott Laboratories
Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.
Bioorg Med Chem Lett 13: 3813-6 (2003)
Merck Frosst Centre For Therapeutic Research
Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.
Bioorg Med Chem Lett 13: 3797-800 (2003)
Wyeth Research
Aryl piperazine melanocortin MC4 receptor agonists.
Bioorg Med Chem Lett 13: 3793-6 (2003)
Neurocrine Biosciences
Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives.
Bioorg Med Chem Lett 13: 3783-7 (2003)
University of Lille
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.
Bioorg Med Chem Lett 13: 3779-82 (2003)
Florida A&M University
The total synthesis of an aurone isolated from Uvaria hamiltonii: aurones and flavones as anticancer agents.
Bioorg Med Chem Lett 13: 3759-63 (2003)
Cardiff University
Exploring selectivity requirements for COX-2 versus COX-1 binding of 3,4-diaryloxazolones using E-state index.
Bioorg Med Chem Lett 13: 3753-7 (2003)
Jadavpur University
A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines.
Bioorg Med Chem Lett 13: 3727-30 (2003)
Pfizer
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.
Bioorg Med Chem Lett 13: 3721-5 (2003)
Pharmacia
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.
Bioorg Med Chem Lett 13: 3715-8 (2003)
Merck
Identification of a novel class of inhibitor of human and Escherichia coli thymidine phosphorylase by in silico screening.
Bioorg Med Chem Lett 13: 3705-9 (2003)
University of Manchester
Biphenyl-based analogues of thiolactomycin, active against Mycobacterium tuberculosis mtFabH fatty acid condensing enzyme.
Bioorg Med Chem Lett 13: 3685-8 (2003)
The University of Birmingham
Biological evaluation of sphingomyelin analogues as inhibitors of sphingomyelinase.
Bioorg Med Chem Lett 13: 3681-4 (2003)
Taisho Pharmaceutical
Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase.
Bioorg Med Chem Lett 13: 3673-7 (2003)
Novartis Research Institute Vienna
Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I.
Bioorg Med Chem Lett 13: 3661-3 (2003)
Imperial College
Identification of potent and novel small-molecule inhibitors of caspase-3.
Bioorg Med Chem Lett 13: 3651-5 (2003)
Sunesis Pharmaceuticals
Design and synthesis of a new fluorescent probe for cytochrome P450 3A4 (CYP 3A4).
Bioorg Med Chem Lett 13: 3643-5 (2003)
University of Basel
Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.
J Pharmacol Exp Ther 307: 947-54 (2003)
Cornell University
Characterization of the transport of the bicyclic peptide phalloidin by human hepatic transport proteins.
Naunyn Schmiedebergs Arch Pharmacol 368: 415-20 (2003)
Deutsches Krebsforschungszentrum
Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators.
J Biol Chem 278: 49773-9 (2003)
Probiodrug
Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line.
Chem Biol 10: 837-46 (2003)
Brigham and Women'S Hospital
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
J Med Chem 46: 4609-24 (2003)
Novartis Institute For Biomedical Research
New prolyl oligopeptidase inhibitors developed from dicarboxylic acid bis(l-prolyl-pyrrolidine) amides.
J Med Chem 46: 4543-51 (2003)
University of Kuopio
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
J Med Chem 46: 4533-42 (2003)
Glaxosmithkline
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues.
J Med Chem 46: 4525-32 (2003)
Glaxosmithkline
Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors.
J Med Chem 46: 4501-15 (2003)
Lindsley F. Kimball Research Institute
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
J Med Chem 46: 4477-86 (2003)
Northwestern University
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.
J Med Chem 46: 4463-76 (2003)
University of London
Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.
J Med Chem 46: 4428-49 (2003)
Glaxosmithkline
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
J Med Chem 46: 4405-18 (2003)
Bristol-Myers Squibb
Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design.
J Med Chem 46: 4393-404 (2003)
Technische Universit£T M£Nchen
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
J Med Chem 46: 4377-92 (2003)
University of Michigan
Biological activity of tropolone.
Biol Pharm Bull 26: 1487-90 (2003)
Osaka Organic Chemical Industry
WAY-855 (3-amino-tricyclo[2.2.1.02.6]heptane-1,3-dicarboxylic acid): a novel, EAAT2-preferring, nonsubstrate inhibitor of high-affinity glutamate uptake.
Br J Pharmacol 140: 839-46 (2003)
Wyeth Research
The structural basis for the selectivity of benzotriazole inhibitors of PTP1B.
Biochemistry 42: 11451-9 (2003)
Merck Research Laboratories
New bioactive diterpene polyesters from Euphorbia decipiens.
J Nat Prod 66: 1221-4 (2003)
University of Karachi
Constituents from the leaves of Phellodendron amurense var. wilsonii and their bioactivity.
J Nat Prod 66: 1207-11 (2003)
National Cheng Kung University
Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.
J Nat Prod 66: 1191-6 (2003)
Kyoto Pharmaceutical University
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Bioorg Med Chem Lett 13: 3623-6 (2003)
Idun Pharmaceuticals
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.
Bioorg Med Chem Lett 13: 3617-22 (2003)
Neurocrine Biosciences
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.
Bioorg Med Chem Lett 13: 3611-6 (2003)
Purdue Pharma
1,2,5,6-tetra-O-benzyl-D-mannitol derivatives as novel HIV protease inhibitors.
Bioorg Med Chem Lett 13: 3601-5 (2003)
Pharmacor
Design and synthesis of novel CCR3 antagonists.
Bioorg Med Chem Lett 13: 3597-600 (2003)
Roche Palo Alto
Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists.
Bioorg Med Chem Lett 13: 3593-6 (2003)
Pfizer
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Bioorg Med Chem Lett 13: 3565-9 (2003)
Georgetown University Medical Center
3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
Bioorg Med Chem Lett 13: 3557-60 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.
Bioorg Med Chem Lett 13: 3541-4 (2003)
Merck Research Laboratories
Synthesis and evaluation of tripeptidyl alpha-ketoamides as human rhinovirus 3C protease inhibitors.
Bioorg Med Chem Lett 13: 3531-6 (2003)
Eli Lilly
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
Bioorg Med Chem Lett 13: 3527-30 (2003)
University of Cape Town
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors.
Bioorg Med Chem Lett 13: 3491-5 (2003)
Pharmacia
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids.
Bioorg Med Chem Lett 13: 3487-90 (2003)
University of Tennessee-Memphis
Pyrimido[1,2-b]-1,2,4,5-tetrazin-6-ones as HCMV protease inhibitors: a new class of heterocycles with flavin-like redox properties.
Bioorg Med Chem Lett 13: 3483-6 (2003)
Wyeth Research
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.
Bioorg Med Chem Lett 13: 3477-82 (2003)
Merck Research Laboratories
An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.
Bioorg Med Chem Lett 13: 3465-70 (2003)
Northwestern University
Synthesis and glycosidase inhibitory activity of some N-substituted 6-deoxy-5a-carba-beta-DL- and L-galactopyranosylamines.
Bioorg Med Chem Lett 13: 3461-3 (2003)
Keio University
Design and synthesis of small chemical inhibitors containing different scaffolds for lck SH2 domain.
Bioorg Med Chem Lett 13: 3455-9 (2003)
Mogam Biotechnology Research Institute
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.
Bioorg Med Chem Lett 13: 3419-21 (2003)
Nps Pharmaceuticals
Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 13: 3405-8 (2003)
Merck Research Laboratories
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
Bioorg Med Chem Lett 13: 3401-4 (2003)
University of Virginia
The rabbit motilin receptor: molecular characterisation and pharmacology.
Br J Pharmacol 140: 948-54 (2003)
Glaxosmithkline
Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.
Mol Pharmacol 64: 865-75 (2003)
The Danish University of Pharmaceutical Sciences
Differential activation of formyl peptide receptor signaling by peptide ligands.
Mol Pharmacol 64: 841-7 (2003)
Pohang University of Science and Technology
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