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Interactions of glycyrrhizin with organic anion transporting polypeptides of rat and human liver.EBI
Hepatol Res 26: 343-347 (2003)
University Of Zurich
N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function.BDB
J Pharmacol Exp Ther 307: 322-30 (2003)
Novartis Pharma
In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates.BDB
J Pharmacol Exp Ther 307: 138-45 (2003)
National Institute On Drug Abuse
The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity.BDB
Chem Biol 10: 705-12 (2003)
Merck Research Laboratories
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.EBI
J Med Chem 46: 4196-204 (2003)
Georgetown University Medical Center
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.EBI
J Med Chem 46: 4188-95 (2003)
Alcon Research
Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.EBI
J Med Chem 46: 4182-7 (2003)
University Of Innsbruck
In vitro analysis of stable, receptor-selective neurotensin[8-13] analogues.EBI
J Med Chem 46: 4141-8 (2003)
Medical University Of South Carolina
Orally active oxime derivatives of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one. Synthesis and pharmacological activity.EBI
J Med Chem 46: 4136-40 (2003)
University Center For Pharmacy
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.EBI
J Med Chem 46: 4104-12 (2003)
Ligand Pharmaceuticals
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.EBI
J Med Chem 46: 4087-103 (2003)
Ligand Pharmaceuticals
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.EBI
J Med Chem 46: 4070-86 (2003)
Glaxosmithkline
Selectivity fields: comparative molecular field analysis (CoMFA) of the glycine/NMDA and AMPA receptors.EBI
J Med Chem 46: 4063-9 (2003)
Moscow State University
Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.BDB
J Med Chem 46: 4050-62 (2003)
Pharmacia
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.EBI
J Med Chem 46: 4043-9 (2003)
Pharmacia
Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process.EBI
J Med Chem 46: 4032-42 (2003)
Università
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.EBI
J Med Chem 46: 4021-31 (2003)
Johnson And Johnson Pharmaceutical Research And Development
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.EBI
J Med Chem 46: 4002-8 (2003)
University Of Maryland
Synthesis and SAR of thrombin inhibitors incorporating a novel 4-amino-morpholinone sscaffold: analysis of X-ray crystal structure of enzyme inhibitor complex.EBI
J Med Chem 46: 3985-4001 (2003)
Link£Ping University
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.EBI
J Med Chem 46: 3975-84 (2003)
Dr. Reddy'S Laboratories
Receptor-mediated targeting of a photosensitizer by its conjugation to gonadotropin-releasing hormone analogues.EBI
J Med Chem 46: 3965-74 (2003)
Institute Of Science
Discovery and preclinical characterization of (+)-3-[4-(1- piperidinoethoxy)phenyl]spiro[indene- 1,1'-indane]-5,5'-diol hydrochloride: a promising nonsteroidal estrogen receptor agonist for hot flush.EBI
J Med Chem 46: 3961-4 (2003)
Dainippon Pharmaceutical
The first potent and selective non-imidazole human histamine H4 receptor antagonists.EBI
J Med Chem 46: 3957-60 (2003)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.EBI
J Med Chem 46: 3953-6 (2003)
Eli Lilly
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.EBI
Bioorg Med Chem Lett 13: 3375-9 (2003)
Neurocrine Biosciences
Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists.EBI
Bioorg Med Chem Lett 13: 3371-4 (2003)
Neurocrine Biosciences
Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists.EBI
Bioorg Med Chem Lett 13: 3367-70 (2003)
Neurocrine Biosciences
Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).EBI
Bioorg Med Chem Lett 13: 3361-5 (2003)
Berlex Biosciences
N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates.EBI
Bioorg Med Chem Lett 13: 3355-9 (2003)
Virginia Commonwealth University
Stereoselective synthesis of phosphoramidate alpha(2-6)sialyltransferase transition-state analogue inhibitors.EBI
Bioorg Med Chem Lett 13: 3351-4 (2003)
Universitaet Konstanz
Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase.EBI
Bioorg Med Chem Lett 13: 3341-4 (2003)
Shire Biochem
Alpha-keto amides as inhibitors of histone deacetylase.EBI
Bioorg Med Chem Lett 13: 3331-5 (2003)
Abbott Laboratories
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.BDB
Bioorg Med Chem Lett 13: 3323-6 (2003)
Merck Research Laboratories
Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.EBI
Bioorg Med Chem Lett 13: 3317-22 (2003)
Neurocrine Biosciences
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 13: 3311-5 (2003)
Neurocrine Biosciences
Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors.EBI
Bioorg Med Chem Lett 13: 3301-3 (2003)
University Of California
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.EBI
Bioorg Med Chem Lett 13: 3297-300 (2003)
Mcgill University/Royal Victoria Hospital
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.EBI
Bioorg Med Chem Lett 13: 3293-6 (2003)
Friedrich-Alexander University
Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression.EBI
Bioorg Med Chem Lett 13: 3277-80 (2003)
Eli Lilly
Synthesis and PDF inhibitory activities of novel benzothiazolylidenehydroxamic acid derivatives.EBI
Bioorg Med Chem Lett 13: 3273-6 (2003)
Senju Pharmaceutical
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.EBI
Bioorg Med Chem Lett 13: 3247-52 (2003)
Purdue Pharma
Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors.EBI
Bioorg Med Chem Lett 13: 3243-6 (2003)
Pfizer
Cyclohexanedione herbicides are inhibitors of rat heart acetyl-CoA carboxylase.EBI
Bioorg Med Chem Lett 13: 3237-42 (2003)
Eli Lilly
Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.EBI
Bioorg Med Chem Lett 13: 3231-5 (2003)
Universidad De Buenos Aires
Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.EBI
Bioorg Med Chem Lett 13: 3203-5 (2003)
Nih
Design and synthesis of fluorinated RXR modulators.EBI
Bioorg Med Chem Lett 13: 3191-5 (2003)
Eli Lilly
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.EBI
Bioorg Med Chem Lett 13: 3185-90 (2003)
Merck Research Laboratories
Regulation of gene expression by synthetic dimerizers with novel specificity.EBI
Bioorg Med Chem Lett 13: 3181-4 (2003)
Ariad Gene Therapeutics
Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands.EBI
Bioorg Med Chem Lett 13: 3177-80 (2003)
Universidad Complutense
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.EBI
Bioorg Med Chem Lett 13: 3171-6 (2003)
University Of Ljubljana
Reversed hydroxamate-bearing thermolysin inhibitors mimic a high-energy intermediate along the enzyme-catalyzed proteolytic reaction pathway.EBI
Bioorg Med Chem Lett 13: 3161-6 (2003)
Pohang University Of Science And Technology
1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 13: 3155-9 (2003)
F. Hoffmann-La Roche
Biological activities of alpha-mangostin derivatives against acidic sphingomyelinase.EBI
Bioorg Med Chem Lett 13: 3151-3 (2003)
Keio University
Analysis of the critical structural determinant(s) of species-selective peroxisome proliferator-activated receptor alpha (PPAR alpha)-activation by phenylpropanoic acid-type PPAR alpha agonists.EBI
Bioorg Med Chem Lett 13: 3145-9 (2003)
Kyorin Pharmaceutical
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors.EBI
Bioorg Med Chem Lett 13: 3129-32 (2003)
Abbott Laboratories
The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors.BDB
J Mol Biol 332: 13-21 (2003)
Morphochem
Potent small molecule inhibitors of spleen tyrosine kinase (Syk).EBI
Bioorg Med Chem Lett 13: 3111-4 (2003)
Aventis Pharmaceuticals
Mapping the kinase domain of Janus Kinase 3.EBI
Bioorg Med Chem Lett 13: 3105-10 (2003)
Aventis Pharmaceuticals
The kinetics of binding to p38MAP kinase by analogues of BIRB 796.EBI
Bioorg Med Chem Lett 13: 3101-4 (2003)
Boehringer Ingelheim Pharmaceuticals
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.EBI
Bioorg Med Chem Lett 13: 3097-100 (2003)
Aventis Pharmaceuticals
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.EBI
Bioorg Med Chem Lett 13: 3091-5 (2003)
Aventis Pharmaceuticals
Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.EBI
Bioorg Med Chem Lett 13: 3087-90 (2003)
Scios
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).EBI
Bioorg Med Chem Lett 13: 3083-6 (2003)
University Of Newcastle
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.BDB
Bioorg Med Chem Lett 13: 3079-82 (2003)
University Of Newcastle
Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.EBI
Bioorg Med Chem Lett 13: 3071-4 (2003)
Ariad Pharmaceuticals
Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.EBI
Bioorg Med Chem Lett 13: 3067-70 (2003)
Ariad Pharmaceuticals
Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.EBI
Bioorg Med Chem Lett 13: 3063-6 (2003)
Ariad Pharmaceuticals
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).BDB
Bioorg Med Chem Lett 13: 3059-62 (2003)
Glaxosmithkline
6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).BDB
Bioorg Med Chem Lett 13: 3055-7 (2003)
Glaxosmithkline
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI
Bioorg Med Chem Lett 13: 3049-53 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.EBI
Bioorg Med Chem Lett 13: 3045-8 (2003)
Ghent University
Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.EBI
Bioorg Med Chem Lett 13: 3041-4 (2003)
Abbott Laboratories
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.EBI
Bioorg Med Chem Lett 13: 3031-4 (2003)
Wyeth Research
Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides.EBI
Bioorg Med Chem Lett 13: 3027-30 (2003)
Instituto De QuíMica MéDica (Csic)
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.BDB
Bioorg Med Chem Lett 13: 3021-6 (2003)
Astrazeneca
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.EBI
Bioorg Med Chem Lett 13: 3015-9 (2003)
Kyoto University
Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration.EBI
Bioorg Med Chem Lett 13: 3005-7 (2003)
Nih
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.EBI
Bioorg Med Chem Lett 13: 3001-4 (2003)
Kyowa Hakko Kogyo
2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors.EBI
Bioorg Med Chem Lett 13: 2993-6 (2003)
Academy Of Sciences Of The Czech Republic
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors.EBI
Bioorg Med Chem Lett 13: 2989-92 (2003)
Academy Of Sciences Of The Czech Republic
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.BDB
Bioorg Med Chem Lett 13: 2985-8 (2003)
Glaxosmithkline
Synthesis of three enantiomeric pairs of scyllo-inositol phosphate and molecular interactions between all possible regioisomers of scyllo-inositol phosphate and inositol 1,4,5-trisphosphate 3-kinase.EBI
Bioorg Med Chem Lett 13: 2981-4 (2003)
Pohang University Of Science & Technology
Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines.EBI
Bioorg Med Chem Lett 13: 2977-80 (2003)
Wyeth Research
Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.BDB
Bioorg Med Chem Lett 13: 2973-6 (2003)
Merck Research Laboratories
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.EBI
Bioorg Med Chem Lett 13: 2967-71 (2003)
Novartis Pharma
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.BDB
Bioorg Med Chem Lett 13: 2961-6 (2003)
Astrazeneca
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.BDB
Bioorg Med Chem Lett 13: 2955-60 (2003)
Astrazeneca
Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: the importance of being neutral.BDB
Bioorg Chem 31: 398-411 (2003)
Johns Hopkins University School Of Medicine
Understanding binding affinity: a combined isothermal titration calorimetry/molecular dynamics study of the binding of a series of hydrophobically modified benzamidinium chloride inhibitors to trypsin.BDB
J Am Chem Soc 125: 10570-9 (2003)
University Of Groningen
10-Methoxydihydrofuscin, fuscinarin, and fuscin, novel antagonists of the human CCR5 receptor from Oidiodendron griseum.EBI
J Nat Prod 66: 1116-7 (2003)
Merlion Pharmaceuticals
CT2108A and B: New fatty acid synthase inhibitors as antifungal agents.EBI
J Nat Prod 66: 1041-6 (2003)
Panlabs
Pyrazole derivatives as partial agonists for the nicotinic acid receptor.EBI
J Med Chem 46: 3945-51 (2003)
Leiden/Amsterdam Center For Drug Research
Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.EBI
J Med Chem 46: 3930-7 (2003)
Virginia Commonwealth University
Synthesis and biological evaluation of novel flavone-8-acetic acid derivatives as reversible inhibitors of aminopeptidase N/CD13.EBI
J Med Chem 46: 3900-13 (2003)
Institut Curie
N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands.EBI
J Med Chem 46: 3883-99 (2003)
Johann Wolfgang Goethe-UniversitäT
Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases.EBI
J Med Chem 46: 3877-82 (2003)
Institute Of Research
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.EBI
J Med Chem 46: 3865-76 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.EBI
J Med Chem 46: 3853-64 (2003)
Universit£
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.EBI
J Med Chem 46: 3840-52 (2003)
Institut De Recherches Servier
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.EBI
J Med Chem 46: 3822-39 (2003)
Universit£
3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.EBI
J Med Chem 46: 3811-21 (2003)
Ghent University
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.EBI
J Med Chem 46: 3778-81 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.EBI
J Med Chem 46: 3775-7 (2003)
Ewha Womans University
Structure-based design of a macrocyclic inhibitor for peptide deformylase.EBI
J Med Chem 46: 3771-4 (2003)
The Ohio State University
Characterization of the role of polar amino acid residues within predicted transmembrane helix 17 in determining the substrate specificity of multidrug resistance protein 3.EBI
Biochemistry 42: 9989-10000 (2003)
Queen'S University
Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines.BDB
Eur J Pharmacol 474: 137-40 (2003)
Harvard University
New potential uroselective NO-donor alpha1-antagonists.EBI
J Med Chem 46: 3762-5 (2003)
Università
Bispyridinium cyclophanes: novel templates for human choline kinase inhibitors.EBI
J Med Chem 46: 3754-7 (2003)
Universidad De Granada
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.EBI
J Med Chem 46: 3728-33 (2003)
University Of Arizona
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.BDB
J Med Chem 46: 3709-27 (2003)
Merck Frosst Centre For Therapeutic Research
A comparison of phosphonothioic acids with phosphonic acids as phosphatase inhibitors.EBI
J Med Chem 46: 3703-8 (2003)
Utah State University
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.EBI
J Med Chem 46: 3655-61 (2003)
Procter & Gamble Pharmaceuticals
Structure-based design and synthesis of novel potent Na+,K+ -ATPase inhibitors derived from a 5alpha,14alpha-androstane scaffold as positive inotropic compounds.EBI
J Med Chem 46: 3644-54 (2003)
Prassis Istituto Di Ricerche Sigma-Tau
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.EBI
J Med Chem 46: 3612-22 (2003)
Lg Life Sciences
Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.EBI
J Med Chem 46: 3581-99 (2003)
Kyorin Pharmaceutical
Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.EBI
J Med Chem 46: 3568-71 (2003)
Universit£
Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein.EBI
J Med Chem 46: 3563-4 (2003)
Institut F£R Molekularbiologie Und Biophysik
Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2.EBI
J Med Chem 46: 3559-62 (2003)
National Institutes Of Health
Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.BDB
Nat Struct Biol 10: 764-9 (2003)
Merck Research Laboratories
A natural product ligand of the oxysterol receptor, liver X receptor.BDB
J Pharmacol Exp Ther 307: 291-6 (2003)
Eli Lilly
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition.BDB
Biochem J 375: 255-62 (2003)
University Of Dundee
[BRCA1 protein expression in sporadic breast and its clinical significance].BDB
Zhonghua Wai Ke Za Zhi 41: 186-8 (2003)
Anhui Medical University
Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist.BDB
Eur J Neurosci 18: 290-5 (2003)
University Of Innsbruck
Acetophenone derivatives from Acronychia pedunculata.EBI
J Nat Prod 66: 990-3 (2003)
National Cheng Kung University
Antiparasitic alkaloids from Psychotria klugii.EBI
J Nat Prod 66: 962-7 (2003)
University Of Mississippi
Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action.EBI
J Nat Prod 66: 954-7 (2003)
Universidad De Chile
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety.EBI
J Med Chem 46: 3555-8 (2003)
Università
Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.EBI
J Med Chem 46: 3526-35 (2003)
Purdue University
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.EBI
J Med Chem 46: 3514-25 (2003)
Pfizer
Development of a water-soluble matrix metalloproteinase inhibitor as an intra-arterial infusion drug for prevention of restenosis after angioplasty.EBI
J Med Chem 46: 3497-501 (2003)
National Cardiovascular Center Research Institute
A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain.EBI
J Med Chem 46: 3483-96 (2003)
Organix
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.EBI
J Med Chem 46: 3463-75 (2003)
Domp&Egrove
Design and synthesis of dihydrofolate reductase inhibitors encompassing a bridging ester group. Evaluation in a mouse colitis model.EBI
J Med Chem 46: 3455-62 (2003)
Uppsala University
Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis.EBI
J Med Chem 46: 3452-4 (2003)
Johns Hopkins University School Of Medicine
Identification of"latent hits" in compound screening collections.EBI
J Med Chem 46: 3441-4 (2003)
Organon Laboratories
Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.EBI
J Med Chem 46: 3437-40 (2003)
Abbott Laboratories
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.EBI
Bioorg Med Chem Lett 13: 2799-803 (2003)
Wyeth Research
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.EBI
Bioorg Med Chem Lett 13: 2795-8 (2003)
Merck Research Laboratories
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.EBI
Bioorg Med Chem Lett 13: 2781-4 (2003)
Merck Research Laboratories
Novel 3-O-acyl mesquitol analogues as free-radical scavengers and enzyme inhibitors: synthesis, biological evaluation and structure-activity relationship.EBI
Bioorg Med Chem Lett 13: 2777-80 (2003)
Institute Of Chemical Technology
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.EBI
Bioorg Med Chem Lett 13: 2773-5 (2003)
Gedeon Richter
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one?EBI
Bioorg Med Chem Lett 13: 2759-63 (2003)
Università
Novel, potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures.EBI
Bioorg Med Chem Lett 13: 2745-8 (2003)
Mrl Rome
Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors.EBI
Bioorg Med Chem Lett 13: 2741-4 (2003)
Hokkaido Collaboration Center
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.EBI
Bioorg Med Chem Lett 13: 2737-40 (2003)
Hokkaido Collaboration Center
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.EBI
Bioorg Med Chem Lett 13: 2719-25 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Structure--activity relationships of the peptide deformylase inhibitor BB-3497: modification of the P2' and P3' side chains.EBI
Bioorg Med Chem Lett 13: 2715-8 (2003)
British Biotech Pharmaceuticals
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the methylene spacer and the P1' side chain.EBI
Bioorg Med Chem Lett 13: 2709-13 (2003)
British Biotech Pharmaceuticals
Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lung.EBI
Bioorg Med Chem Lett 13: 2687-92 (2003)
University Of Mainz
Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors.EBI
Bioorg Med Chem Lett 13: 2659-62 (2003)
Universit£
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.EBI
Bioorg Med Chem Lett 13: 2655-8 (2003)
The University Of Tokyo
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).EBI
Bioorg Med Chem Lett 13: 2647-50 (2003)
University Of Cincinnati
Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 2625-8 (2003)
Astrazeneca R&D Charnwood
GABA(C) receptors as drug targets.BDB
Curr Drug Targets CNS Neurol Disord 2: 260-8 (2003)
University Of Sydney
High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II.BDB
J Comb Chem 5: 456-64 (2003)
Uppsala University
2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis.EBI
Bioorg Med Chem Lett 13: 2591-4 (2003)
Wyeth Research
Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.EBI
Bioorg Med Chem Lett 13: 2587-90 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide.EBI
Bioorg Med Chem Lett 13: 2583-6 (2003)
Kyowa Hakko Kogyo
Tripeptide inhibitors of Yersinia protein-tyrosine phosphatase.EBI
Bioorg Med Chem Lett 13: 2577-81 (2003)
National Cancer Institute-Frederick
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.BDB
Bioorg Med Chem Lett 13: 2573-6 (2003)
Merck Research Laboratories
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.BDB
Bioorg Med Chem Lett 13: 2569-72 (2003)
Merck Research Laboratories
Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor.EBI
Bioorg Med Chem Lett 13: 2565-8 (2003)
Virginia Commonwealth University
Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors.EBI
Bioorg Med Chem Lett 13: 2561-3 (2003)
Inha University
Effect of structural modification on the inhibitory selectivity of rutaecarpine derivatives on human CYP1A1, CYP1A2, and CYP1B1.EBI
Bioorg Med Chem Lett 13: 2535-8 (2003)
National Research Institute Of Chinese Medicine
Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones.EBI
Bioorg Med Chem Lett 13: 2513-8 (2003)
Guilford Pharmaceuticals
3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators.EBI
Bioorg Med Chem Lett 13: 2509-12 (2003)
University Of California
2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 2497-500 (2003)
Neurogen
High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate.EBI
Bioorg Med Chem Lett 13: 2493-6 (2003)
Mcmaster University
Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.BDB
Bioorg Med Chem Lett 13: 2485-8 (2003)
Merck Research Laboratories
Development of 3D-QSAR models in cyclic ureidobenzenesulfonamides: human beta3-adrenergic receptor agonist.EBI
Bioorg Med Chem Lett 13: 2481-4 (2003)
Central Drug Research Institute
Comparative molecular field analysis (CoMFA) of phthalazine derivatives as phosphodiesterase IV inhibitors.EBI
Bioorg Med Chem Lett 13: 2473-9 (2003)
National Institute Of Pharmaceutical Education And Research
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.BDB
Bioorg Med Chem Lett 13: 2465-8 (2003)
Hoffmann-La Roche
Effect of catechol derivatives on cell growth and lipoxygenase activity.EBI
Bioorg Med Chem Lett 13: 2435-9 (2003)
Aston University
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.EBI
J Med Chem 46: 3412-23 (2003)
Industrial Research
Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors.EBI
J Med Chem 46: 3403-11 (2003)
Washington University
Novel benzylidene-9(10H)-anthracenones as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization.EBI
J Med Chem 46: 3382-94 (2003)
Westphalian Wilhelms-University
Tethered dimers as NAD synthetase inhibitors with antibacterial activity.EBI
J Med Chem 46: 3371-81 (2003)
University Of Alabama At Birmingham
Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors.EBI
J Med Chem 46: 3354-70 (2003)
F. Hoffmann-La Roche
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.EBI
J Med Chem 46: 3333-41 (2003)
Novo Nordisk
Computer-aided selection of potential antihypertensive compounds with dual mechanism of action.EBI
J Med Chem 46: 3326-32 (2003)
Institute Of Biomedical Chemistry Of Russian Academy Of Medical Sciences
A computational model of binding thermodynamics: the design of cyclin-dependent kinase 2 inhibitors.EBI
J Med Chem 46: 3314-25 (2003)
University Of California
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.EBI
J Med Chem 46: 3292-9 (2003)
National Cancer Institute-Frederick
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.EBI
J Med Chem 46: 3257-74 (2003)
Glaxosmithkline
l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance.EBI
J Med Chem 46: 3245-56 (2003)
The University Of Georgia
Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.EBI
J Med Chem 46: 3230-44 (2003)
Eberhard-Karls-University T£Bingen
Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'.EBI
J Med Chem 46: 3221-9 (2003)
National Hellenic Research Foundation
Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.EBI
J Med Chem 46: 3201-9 (2003)
Kobe Gakuin University
(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.EBI
J Med Chem 46: 3197-200 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
First dual aromatase-steroid sulfatase inhibitors.BDB
J Med Chem 46: 3193-6 (2003)
University Of Bath
Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine.EBI
J Med Chem 46: 3189-92 (2003)
Eli Lilly
Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.BDB
J Chem Neuroanat 25: 233-47 (2003)
University Of Michigan
Asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine: preparation, resolution and biological activities toward insects and their nerve preparations.EBI
Biosci Biotechnol Biochem 67: 980-8 (2003)
Gifu University
Pochonins A-F, new antiviral and antiparasitic resorcylic acid lactones from Pochonia chlamydosporia var. catenulata.EBI
J Nat Prod 66: 829-37 (2003)
Bayer Healthcare
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.EBI
J Nat Prod 66: 739-42 (2003)
University Of Karachi
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.EBI
J Med Chem 46: 3174-7 (2003)
University Of Bath
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.EBI
J Med Chem 46: 3162-5 (2003)
Osaka University
Structural determinants of selective thyromimetics.EBI
J Med Chem 46: 3152-61 (2003)
University Of California
Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.EBI
J Med Chem 46: 3138-51 (2003)
Guilford Pharmaceuticals
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.EBI
J Med Chem 46: 3127-37 (2003)
Research Triangle Institute
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.EBI
J Med Chem 46: 3116-26 (2003)
Seoul National University
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.EBI
J Med Chem 46: 3102-8 (2003)
Università
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.EBI
J Med Chem 46: 3060-71 (2003)
Eli Lilly
Histamine-releasing activity and binding to the FcepsilonRI alpha human mast cell receptor subunit of mast cell degranulating peptide analogues with alanine substitutions.EBI
J Med Chem 46: 3008-12 (2003)
Mount Sinai School Of Medicine
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.EBI
J Med Chem 46: 2973-84 (2003)
Merck Research Laboratories
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.BDB
J Med Chem 46: 2945-57 (2003)
Novartis Pharmaceuticals
A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents.EBI
J Med Chem 46: 2932-44 (2003)
University Of Illinois At Urbana-Champaign
Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.EBI
J Med Chem 46: 2917-31 (2003)
Institut FüR Molekulare Physiologie
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.EBI
J Med Chem 46: 2908-16 (2003)
National Institute On Drug Abuse
New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes.EBI
J Med Chem 46: 2877-94 (2003)
Universit£
Docking and database screening reveal new classes of Plasmodium falciparum dihydrofolate reductase inhibitors.EBI
J Med Chem 46: 2834-45 (2003)
Università
Dihydrofolate reductase mutant with exceptional resistance to methotrexate but not to trimetrexate.EBI
J Med Chem 46: 2816-8 (2003)
University Of Minnesota
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).EBI
J Med Chem 46: 2795-812 (2003)
Virginia Commonwealth University
Novel IKK inhibitors: beta-carbolines.EBI
Bioorg Med Chem Lett 13: 2419-22 (2003)
Millennium Pharmaceuticals
Identification of oxidation product of arbutin in mushroom tyrosinase assay system.EBI
Bioorg Med Chem Lett 13: 2409-12 (2003)
University Of California
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.BDB
Bioorg Med Chem Lett 13: 2405-8 (2003)
Bristol-Myers Squibb
Constrained phytoestrogens and analogues as ERbeta selective ligands.EBI
Bioorg Med Chem Lett 13: 2399-403 (2003)
Wyeth Research
Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2.EBI
Bioorg Med Chem Lett 13: 2393-7 (2003)
Eli Lilly
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.EBI
Bioorg Med Chem Lett 13: 2389-91 (2003)
Cnrs
Synthesis and inhibitory activity of ubiquinone-acetogenin hybrid inhibitor with bovine mitochondrial complex I.EBI
Bioorg Med Chem Lett 13: 2385-8 (2003)
Kyoto University
Novel inhibitors of procollagen C-proteinase. Part 2: glutamic acid hydroxamates.EBI
Bioorg Med Chem Lett 13: 2381-4 (2003)
Combichem
Synthesis and biological testing of non-fluorinated analogues of levofloxacin.EBI
Bioorg Med Chem Lett 13: 2373-5 (2003)
Procter & Gamble Pharmaceuticals
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.EBI
Bioorg Med Chem Lett 13: 2369-72 (2003)
Pharmacia
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.EBI
Bioorg Med Chem Lett 13: 2363-7 (2003)
Pharmacia
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.EBI
Bioorg Med Chem Lett 13: 2355-8 (2003)
Lead Gene
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.EBI
Bioorg Med Chem Lett 13: 2347-50 (2003)
Tanabe Seiyaku
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.EBI
Bioorg Med Chem Lett 13: 2341-5 (2003)
Tanabe Seiyaku
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).EBI
Bioorg Med Chem Lett 13: 2337-40 (2003)
Amgen
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3.EBI
Bioorg Med Chem Lett 13: 2331-6 (2003)
Pfizer
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.EBI
Bioorg Med Chem Lett 13: 2319-25 (2003)
Pharmacia
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.EBI
Bioorg Med Chem Lett 13: 2307-10 (2003)
Abbott Laboratories
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.EBI
Bioorg Med Chem Lett 13: 2297-302 (2003)
Boehringer Ingelheim Pharma
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI
Bioorg Med Chem Lett 13: 2291-5 (2003)
Boehringer Ingelheim Pharma
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.EBI
Bioorg Med Chem Lett 13: 2281-4 (2003)
University Of Sydney
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.BDB
Bioorg Med Chem Lett 13: 2261-7 (2003)
Eli Lilly
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).BDB
Biochem J 374: 639-46 (2003)
University Of Padova
Complexation and chiral recognition thermodynamics of gamma-cyclodextrin with N-acetyl- and N-carbobenzyloxy-dipeptides possessing two aromatic rings.BDB
J Org Chem 68: 5228-35 (2003)
Japan Science And Technology Agency
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.BDB
Mol Pharmacol 64: 143-53 (2003)
Abbott Laboratories
Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.EBI
J Med Chem 46: 2790-3 (2003)
National Cancer Institute-Frederick
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.EBI
J Med Chem 46: 2774-89 (2003)
Novartis Institute For Biomedical Research
Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents.EBI
J Med Chem 46: 2740-54 (2003)
University Of Pittsburgh
Synthesis of substituted 6-anilinouracils and their inhibition of DNA polymerase IIIC and Gram-positive bacterial growth.EBI
J Med Chem 46: 2731-9 (2003)
Glsynthesis
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.EBI
J Med Chem 46: 2716-30 (2003)
University Of Vermont
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.EBI
J Med Chem 46: 2683-96 (2003)
Ligand Pharmaceuticals
The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.EBI
J Med Chem 46: 2641-55 (2003)
Wroclaw University Of Technology
Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae.EBI
J Med Chem 46: 2631-40 (2003)
Chinese Academy Of Sciences
Utilization of a beta-aminophosphotyrosyl mimetic in the design and synthesis of macrocyclic Grb2 SH2 domain-binding peptides.EBI
J Med Chem 46: 2621-30 (2003)
National Cancer Institute-Frederick
Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors.EBI
J Med Chem 46: 2606-20 (2003)
Umr C8076 (Cnrs)
Characterization of a series of 3-amino-2-phenylpropene derivatives as novel bovine chromaffin vesicular monoamine transporter inhibitors.EBI
J Med Chem 46: 2599-605 (2003)
Wichita State University
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.EBI
J Med Chem 46: 2589-98 (2003)
Nida-Irp
Inhibition of Cdc25 phosphatases by indolyldihydroxyquinones.EBI
J Med Chem 46: 2580-8 (2003)
Duke University
QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes.EBI
J Med Chem 46: 2572-9 (2003)
Uppsala University
Spirocyclopropyl beta-lactams as mechanism-based inhibitors of serine beta-lactamases. Synthesis by rhodium-catalyzed cyclopropanation of 6-diazopenicillanate sulfone.EBI
J Med Chem 46: 2569-71 (2003)
Wyeth Research
Borrelidin induces the transcription of amino acid biosynthetic enzymes via a GCN4-dependent pathway.EBI
Bioorg Med Chem Lett 13: 2235-7 (2003)
Boston University
Discovery of a potent and selective series of pyrazole bacterial methionyl-tRNA synthetase inhibitors.EBI
Bioorg Med Chem Lett 13: 2231-4 (2003)
Cubist Pharmaceutical
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.EBI
Bioorg Med Chem Lett 13: 2217-22 (2003)
Indiana University School Of Medicine
4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor.EBI
Bioorg Med Chem Lett 13: 2211-5 (2003)
Pfizer
6-Alkyl, alkoxy, or alkylthio-substituted 3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 13: 2205-9 (2003)
University Of Alberta
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.EBI
Bioorg Med Chem Lett 13: 2199-203 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.EBI
Bioorg Med Chem Lett 13: 2195-8 (2003)
Wyeth Research
Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists.EBI
Bioorg Med Chem Lett 13: 2191-4 (2003)
Wyeth Research
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.EBI
Bioorg Med Chem Lett 13: 2179-83 (2003)
National Institute On Drug Abuse-Intramural Research Program
Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.EBI
Bioorg Med Chem Lett 13: 2173-7 (2003)
National Cancer Institute-Frederick
Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2.EBI
Bioorg Med Chem Lett 13: 2167-72 (2003)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Bivalent biogenic amine reuptake inhibitors.EBI
Bioorg Med Chem Lett 13: 2151-4 (2003)
Human Biomolecular Research Institute
Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.EBI
Bioorg Med Chem Lett 13: 2145-9 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Nicotinyl aspartyl ketones as inhibitors of caspase-3.BDB
Bioorg Med Chem Lett 13: 2137-40 (2003)
Merck Frosst Canada
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.EBI
Bioorg Med Chem Lett 13: 2131-5 (2003)
Abbott Laboratories
2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships.EBI
Bioorg Med Chem Lett 13: 2113-8 (2003)
Glaxosmithkline
Novel inhibitors of procollagen C-terminal proteinase. Part 1: diamino Acid hydroxamates.EBI
Bioorg Med Chem Lett 13: 2101-4 (2003)
Combichem
Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.EBI
Bioorg Med Chem Lett 13: 2097-100 (2003)
Guilford Pharmaceuticals
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.BDB
Neuropsychopharmacology 28: 1400-11 (2003)
Case Western Reserve University
Urea small molecule agonists on mouse melanocortin receptors.EBI
Bioorg Med Chem Lett 13: 2079-82 (2003)
University Of Florida
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.EBI
Bioorg Med Chem Lett 13: 2075-8 (2003)
Ligand Pharmaceuticals
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.EBI
Bioorg Med Chem Lett 13: 2071-4 (2003)
Ligand Pharmaceuticals
Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.EBI
Bioorg Med Chem Lett 13: 2059-63 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.EBI
Bioorg Med Chem Lett 13: 2055-8 (2003)
Pfizer
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.EBI
Bioorg Med Chem Lett 13: 2051-3 (2003)
Ligand Pharmaceuticals
Inhibition of mandelate racemase by alpha-fluorobenzylphosphonates.EBI
Bioorg Med Chem Lett 13: 2041-4 (2003)
Dalhousie University
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).EBI
Bioorg Med Chem Lett 13: 2035-40 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.EBI
Bioorg Med Chem Lett 13: 2029-33 (2003)
Basf
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).EBI
Bioorg Med Chem Lett 13: 2021-4 (2003)
Organon K.K.
The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles.EBI
Bioorg Med Chem Lett 13: 2003-7 (2003)
Abbott Laboratories
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.EBI
Bioorg Med Chem Lett 13: 1997-2001 (2003)
Novartis Pharma
The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V).EBI
Bioorg Med Chem Lett 13: 1993-6 (2003)
The University Of Georgia
Structure-activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles, core-modified analogues and amide isosteres.EBI
Bioorg Med Chem Lett 13: 1989-92 (2003)
Pfizer
Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside.EBI
Bioorg Med Chem Lett 13: 1985-8 (2003)
Georgia Institute Of Technology
Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.EBI
Bioorg Med Chem Lett 13: 1981-4 (2003)
Schering
Hemisynthesis and preliminary evaluation of novel endocannabinoid analogues.EBI
Bioorg Med Chem Lett 13: 1977-80 (2003)
Umr Cnrs 5074
Sphingomyelin analogues as inhibitors of sphingomyelinase.EBI
Bioorg Med Chem Lett 13: 1963-6 (2003)
Taisho Pharmaceutical
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.EBI
Bioorg Med Chem Lett 13: 1959-61 (2003)
The Schering Plough Research Institute
Analysis of 6-(2,2-Dichloroacetamido)chrysene interaction with the hypoxanthine phosphoribosyltransferase from Trypanosoma cruzi.EBI
J Med Chem 46: 2548-50 (2003)
University Of Connecticut
Synthesis and antitumor activity of novel O-carbamoylmethyloxime derivatives of radicicol.EBI
J Med Chem 46: 2534-41 (2003)
Pharmaceutical Research Institute
Design, synthesis, and evaluation of analogues of 3,3,3-trifluoro-2-hydroxy-2-phenyl-propionamide as orally available general anesthetics.EBI
J Med Chem 46: 2494-501 (2003)
University Of Virginia
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.BDB
J Med Chem 46: 2482-93 (2003)
Sapienza University Of Rome
Discovery and structure-activity relationships of novel piperidine inhibitors of farnesyltransferase.EBI
J Med Chem 46: 2467-73 (2003)
Pharmaceutical Research Institute
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives.EBI
J Med Chem 46: 2446-55 (2003)
Shionogi
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.EBI
J Med Chem 46: 2436-45 (2003)
Shionogi
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.EBI
J Med Chem 46: 2413-26 (2003)
Merck Frosst Centre For Therapeutic Research
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.EBI
J Med Chem 46: 2404-12 (2003)
Abbott
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.EBI
J Med Chem 46: 2376-96 (2003)
Wyeth Research
Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.EBI
J Med Chem 46: 2361-75 (2003)
Wyeth Research
Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors.EBI
J Med Chem 46: 2352-60 (2003)
Università
Three dimensional pharmacophore modeling of human CYP17 inhibitors. Potential agents for prostate cancer therapy.EBI
J Med Chem 46: 2345-51 (2003)
Accelrys
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.EBI
J Med Chem 46: 2334-44 (2003)
Novartis Pharma
Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening.EBI
J Med Chem 46: 2304-12 (2003)
F. Hoffmann-La Roche
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.BDB
J Med Chem 46: 2283-6 (2003)
Pfizer
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.BDB
J Med Chem 46: 2279-82 (2003)
University Of Bologna
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.EBI
J Med Chem 46: 2261-70 (2003)
Technische Universit£T Darmstadt
Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates.BDB
Biochem Biophys Res Commun 305: 909-14 (2003)
St. Mary'S Hospital
Isolation and synthesis of a new bioactive ellagic acid derivative from Combretum yunnanensis.EBI
J Nat Prod 66: 729-31 (2003)
Teikyo University
New sesquiterpene quinols from a Micronesian sponge, Aka sp.EBI
J Nat Prod 66: 686-9 (2003)
University Of Oklahoma
Brominated polyacetylenes from the Philippines sponge Diplastrella sp.EBI
J Nat Prod 66: 667-70 (2003)
University Of California At San Diego
Developmental expression of heteromeric nicotinic receptor subtypes in chick retina.BDB
Mol Pharmacol 63: 1329-37 (2003)
University Of Milan
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.BDB
Mol Pharmacol 63: 1223-9 (2003)
Case Western Reserve University
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.BDB
Life Sci 73: 371-9 (2003)
Merck Research Laboratories
The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways.BDB
J Pharmacol Exp Ther 306: 954-64 (2003)
Institut De Recherches Servier
Synthesis and SAR of cis-1-benzoyl-1,2,3,4-tetrahydroquinoline ligands for control of gene expression in ecdysone responsive systems.EBI
Bioorg Med Chem Lett 13: 1943-6 (2003)
Rheogene
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.BDB
Bioorg Med Chem Lett 13: 1939-42 (2003)
Sugen
Antifungal activity of a Candida albicans GGTase I inhibitor-alanine conjugate. Inhibition of Rho1p prenylation in C. albicans.EBI
Bioorg Med Chem Lett 13: 1935-7 (2003)
Gpc Biotech
Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.EBI
Bioorg Med Chem Lett 13: 1931-4 (2003)
Neurocrine Biosciences
6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain.EBI
Bioorg Med Chem Lett 13: 1927-30 (2003)
Neurocrine Biosciences
Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.EBI
Bioorg Med Chem Lett 13: 1923-6 (2003)
Merck Frosst Centre For Therapeutic Research
A novel estrogen receptor ligand template.EBI
Bioorg Med Chem Lett 13: 1919-22 (2003)
Bayer
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.EBI
Bioorg Med Chem Lett 13: 1911-4 (2003)
Rensselaer Polytechnic Institute
Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).EBI
Bioorg Med Chem Lett 13: 1907-10 (2003)
Eli Lilly
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.EBI
Bioorg Med Chem Lett 13: 1903-5 (2003)
Eli Lilly
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.EBI
Bioorg Med Chem Lett 13: 1897-901 (2003)
Abbott Laboratories
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.EBI
Bioorg Med Chem Lett 13: 1891-5 (2003)
Merck Research Laboratories
Potent, selective inhibitors of protein tyrosine phosphatase 1B.BDB
Bioorg Med Chem Lett 13: 1887-90 (2003)
Abbott Laboratories
Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression.EBI
Bioorg Med Chem Lett 13: 1883-6 (2003)
Rheogene
Design and synthesis of novel pyrrolidine-containing bradykinin antagonists.EBI
Bioorg Med Chem Lett 13: 1879-82 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.EBI
Bioorg Med Chem Lett 13: 1873-8 (2003)
Roche Bioscience
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).EBI
Bioorg Med Chem Lett 13: 1865-8 (2003)
Universit£
Amide analogues of TSA: synthesis, binding mode analysis and HDAC inhibition.EBI
Bioorg Med Chem Lett 13: 1861-4 (2003)
Vrije Universiteit Brussel
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.EBI
Bioorg Med Chem Lett 13: 1857-9 (2003)
Eli Lilly
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).EBI
J Med Chem 46: 2246-9 (2003)
The Danish University Of Pharmaceutical Sciences
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.EBI
J Med Chem 46: 2227-40 (2003)
Merck Sharp & Dohme Research Laboratories
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.EBI
J Med Chem 46: 2216-26 (2003)
University Of North Carolina At Chapel Hill
Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin-4-ylmethyl]amine.EBI
J Med Chem 46: 2205-15 (2003)
Wayne State University
Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors.EBI
J Med Chem 46: 2197-204 (2003)
University Of Montpellier
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.BDB
J Med Chem 46: 2187-96 (2003)
University Of Agricultural Sciences And Veterinary Medicine
Metal coordination-based inhibitors of adenylyl cyclase: novel potent P-site antagonists.EBI
J Med Chem 46: 2177-86 (2003)
Millennium Pharmaceuticals
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.EBI
J Med Chem 46: 2169-76 (2003)
Universit£
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein.EBI
J Med Chem 46: 2152-68 (2003)
Pfizer
Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.EBI
J Med Chem 46: 2117-24 (2003)
Universit£
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.EBI
J Med Chem 46: 2110-6 (2003)
Bristol-Myers Squibb
Structure-activity relationships of dynorphin a analogues modified in the address sequence.EBI
J Med Chem 46: 2104-9 (2003)
University Of California
Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.BDB
J Med Chem 46: 2093-103 (2003)
Abbott Laboratories
Binding structures and potencies of oxidosqualene cyclase inhibitors with the homologous squalene-hopene cyclase.EBI
J Med Chem 46: 2083-92 (2003)
Albert-Ludwigs-University Of Freiburg
Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method.EBI
J Med Chem 46: 2074-82 (2003)
Johnson & Johnson Pharmaceutical Research And Development
3D QSAR analyses-guided rational design of novel ligands for the (alpha4)2(beta2)3 nicotinic acetylcholine receptor.EBI
J Med Chem 46: 2031-48 (2003)
Institut F£R Pharmazeutische Chemie Der Philipps-Universit£T Marburg
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.BDB
J Med Chem 46: 2027-30 (2003)
Eli Lilly
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.EBI
J Med Chem 46: 2023-6 (2003)
Neurocrine Biosciences
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.EBI
J Med Chem 46: 2017-22 (2003)
Aventis Pharmaceuticals
Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.BDB
J Mol Biol 329: 93-120 (2003)
Celera
Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.BDB
J Comb Chem 5: 336-44 (2003)
University Of Anterwerp
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.EBI
Pharm Res 20: 537-44 (2003)
Schering-Plough Research Institute
Thermodynamic characterization of the binding of nucleotides to glycyl-tRNA synthetase.BDB
Biochemistry 42: 5333-40 (2003)
Medical College Of Ohio
Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches.EBI
Bioorg Med Chem Lett 13: 1829-35 (2003)
Aventis Pharmaceuticals
Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives.EBI
Bioorg Med Chem Lett 13: 1825-7 (2003)
Instituto PolitéCnico Nacional
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.EBI
Bioorg Med Chem Lett 13: 1821-4 (2003)
Merck Research Laboratories
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.EBI
Bioorg Med Chem Lett 13: 1809-12 (2003)
Merck Research Laboratories
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.EBI
Bioorg Med Chem Lett 13: 1801-4 (2003)
Merck Research Laboratories
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.EBI
Bioorg Med Chem Lett 13: 1795-9 (2003)
Bristol-Myers Squibb
A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp.EBI
Bioorg Med Chem Lett 13: 1791-4 (2003)
Schering-Plough Research Institute
Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives.EBI
Bioorg Med Chem Lett 13: 1783-6 (2003)
Université
Non-imidazole heterocyclic histamine H3 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1767-70 (2003)
Johnson & Johnson Pharmaceutical Research And Development
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1759-62 (2003)
F. Hoffmann-La Roche
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.EBI
Bioorg Med Chem Lett 13: 1741-4 (2003)
Abbott Laboratories
Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.EBI
Bioorg Med Chem Lett 13: 1729-32 (2003)
Peking University
Solid-phase synthesis of endothelin receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1721-4 (2003)
Basf
New fibrinolytic agents: benzothiophene derivatives as inhibitors of the t-PA-PAI-1 complex formation.EBI
Bioorg Med Chem Lett 13: 1705-8 (2003)
Institut De Recherches Servier
Discovery of novel low molecular weight inhibitors of IMPDH via virtual needle screening.EBI
Bioorg Med Chem Lett 13: 1691-4 (2003)
Roche Discovery Welwyn
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.BDB
Bioorg Med Chem Lett 13: 1673-7 (2003)
Merck Research Laboratories
Inactivation of S-adenosyl-L-homocysteine hydrolase with novel 5'-thioadenosine derivatives. Antiviral effects.EBI
Bioorg Med Chem Lett 13: 1649-52 (2003)
Umr 6519
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 13: 1639-43 (2003)
Dr. Reddy'S Laboratories
Structure-activity relationship on human serum paraoxonase (PON1) using substrate analogues and inhibitors.EBI
Bioorg Med Chem Lett 13: 1623-6 (2003)
The University Of Birmingham
Synthesis and tyrosinase inhibitory activity of novel N-hydroxybenzyl-N-nitrosohydroxylamines.BDB
Bioorg Chem 31: 129-35 (2003)
Keio University
Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition.BDB
Chem Biol 10: 341-9 (2003)
University Of North Carolina At Chapel Hill
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.EBI
J Med Chem 46: 2008-16 (2003)
Vrije Universiteit
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.EBI
J Med Chem 46: 1997-2007 (2003)
Georgetown University Medical Center
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.EBI
J Med Chem 46: 1989-96 (2003)
Guilford Pharmaceuticals
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.EBI
J Med Chem 46: 1980-8 (2003)
Hokkaido University
Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.EBI
J Med Chem 46: 1962-79 (2003)
Université
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.EBI
J Med Chem 46: 1940-7 (2003)
National Cancer Institute-Frederick
Design of selective peptidomimetic agonists for the human orphan receptor BRS-3.EBI
J Med Chem 46: 1918-30 (2003)
Technische UniversitäT MüNchen
Antiviral amphipathic oligo- and polyribonucleotides: analogue development and biological studies.EBI
J Med Chem 46: 1878-85 (2003)
University Of Utah
2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications.EBI
J Med Chem 46: 1870-7 (2003)
Deakin University
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.EBI
J Med Chem 46: 1858-69 (2003)
University Of Pennsylvania
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.EBI
J Med Chem 46: 1845-57 (2003)
Ajinomoto
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.BDB
J Med Chem 46: 1831-44 (2003)
University Of Pennsylvania
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.EBI
J Med Chem 46: 1811-23 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzodiazepines as potent and selective bradykinin B1 antagonists.EBI
J Med Chem 46: 1803-6 (2003)
Merck Research Laboratories
Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase.EBI
J Med Chem 46: 1799-802 (2003)
Elan Pharmaceuticals
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.EBI
J Med Chem 46: 1775-94 (2003)
Research Triangle Institute
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.BDB
J Pharmacol Exp Ther 306: 377-86 (2003)
Pudue Pharma Discovery Research
Dihydropiperazine neonicotinoid compounds. Synthesis and insecticidal activity.EBI
J Agric Food Chem 51: 3035-42 (2003)
Dow Agrosciences
Identification and characterization of a novel RF-amide peptide ligand for orphan G-protein-coupled receptor SP9155.BDB
J Biol Chem 278: 27652-7 (2003)
Schering-Plough Research Institute
Callysponginol sulfate A, an MT1-MMP inhibitor isolated from the marine sponge Callyspongia truncata.EBI
J Nat Prod 66: 569-71 (2003)
The University Of Tokyo
Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.EBI
J Nat Prod 66: 551-3 (2003)
Merck Research Laboratories
Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria lateriflora.EBI
J Nat Prod 66: 535-7 (2003)
Tom'S Of Maine
Insights into antifolate resistance from malarial DHFR-TS structures.BDB
Nat Struct Biol 10: 257-65 (2003)
Mahidol University
Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram.BDB
J Pharmacol Exp Ther 305: 565-72 (2003)
University Of Tennessee
Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein.EBI
AIDS 17: 1092-4 (2003)
Tufts University School Of Medicine
The selective inhibition of phosphatases by natural toxins: the anhydride domain of tautomycin is not a primary factor in controlling PP1/PP2A selectivity.EBI
Bioorg Med Chem Lett 13: 1597-600 (2003)
University Of California Irvine
Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter.EBI
Bioorg Med Chem Lett 13: 1591-5 (2003)
Wayne State University
New scaffolds in the development of mu opioid-receptor ligands.EBI
Bioorg Med Chem Lett 13: 1585-9 (2003)
Astrazeneca R&D Montreal
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).BDB
Bioorg Med Chem Lett 13: 1581-4 (2003)
Glaxosmithkline
5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).BDB
Bioorg Med Chem Lett 13: 1577-80 (2003)
Glaxosmithkline
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.EBI
Bioorg Med Chem Lett 13: 1571-4 (2003)
Abbott Laboratories
Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam.EBI
Bioorg Med Chem Lett 13: 1561-4 (2003)
University Of Montpellier
Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.EBI
Bioorg Med Chem Lett 13: 1553-5 (2003)
Ufr Des Sciences Pharmaceutiques
Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1549-52 (2003)
Sookmyung Women'S University
5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.EBI
Bioorg Med Chem Lett 13: 1543-7 (2003)
Johnson & Johnson Pharmaceutical Research & Development
A novel metal-chelating inhibitor of protein farnesyltransferase.EBI
Bioorg Med Chem Lett 13: 1523-6 (2003)
Kumamoto University
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.EBI
Bioorg Med Chem Lett 13: 1517-21 (2003)
Glaxosmithkline
Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.EBI
Bioorg Med Chem Lett 13: 1513-5 (2003)
Genentech
Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.EBI
J Med Chem 46: 1769-72 (2003)
Neurocrine Biosciences
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.EBI
J Med Chem 46: 1764-8 (2003)
Kyoto University
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.EBI
J Med Chem 46: 1758-63 (2003)
University Of Innsbruck
Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.EBI
J Med Chem 46: 1726-36 (2003)
Harvard Medical School
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.EBI
J Med Chem 46: 1716-25 (2003)
F. Hoffmann-La Roche
Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A.EBI
J Med Chem 46: 1670-82 (2003)
Purdue University
Aromatic reduced amide bond peptidomimetics as selective inhibitors of neuronal nitric oxide synthase.EBI
J Med Chem 46: 1661-9 (2003)
Northwestern University
An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study.BDB
J Med Chem 46: 1636-44 (2003)
Academy Of Sciences Of The Czech Republic
Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.BDB
J Med Chem 46: 1627-35 (2003)
Glaxosmithkline
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.BDB
J Med Chem 46: 1580-8 (2003)
Karo Bio
Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).EBI
J Med Chem 46: 1571-9 (2003)
National Cancer Institute-Frederick
Pharmacological studies of thyrotropin-releasing hormone (TRH) receptors from Xenopus laevis: is xTRHR3 a TRH receptor?BDB
Endocrinology 144: 1842-6 (2003)
National Institute Of Diabetes And Digestive And Kidney Diseases
Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5.EBI
Mol Pharmacol 63: 1094-103 (2003)
The Netherlands Cancer Institute
[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.BDB
Mol Pharmacol 63: 1082-93 (2003)
Johnson And Johnson Pharmaceutical Research And Development, Beerse
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.BDB
Eur J Biochem 270: 1746-58 (2003)
Uppsala University
Design, synthesis and in vitro evaluation of novel derivatives as serotonin N-acetyltransferase inhibitors.BDB
J Enzyme Inhib Med Chem 17: 409-14 (2002)
UniversitÉ
SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation.BDB
J Pharmacol Exp Ther 306: 407-20 (2003)
Sanofi-Synthelabo Research
Interactions of human organic anion as well as cation transporters with indoxyl sulfate.EBI
Eur J Pharmacol 466: 13-20 (2003)
Nagoya University School Of Medicine
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.EBI
J Med Chem 46: 1563-6 (2003)
University Of Bath
Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate.EBI
J Med Chem 46: 1538-45 (2003)
Organix
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.EBI
J Med Chem 46: 1523-30 (2003)
Freie Universit£T Berlin
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.EBI
J Med Chem 46: 1512-22 (2003)
Universidad Complutense
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.EBI
J Med Chem 46: 1492-503 (2003)
Leiden University
Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity.EBI
J Med Chem 46: 1484-91 (2003)
Free University Of Berlin
Kinase inhibitors: not just for kinases anymore.EBI
J Med Chem 46: 1478-83 (2003)
Northwestern University
Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.EBI
J Med Chem 46: 1465-9 (2003)
Niddk
Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors.EBI
J Med Chem 46: 1456-64 (2003)
Georgia Institute Of Technology
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.EBI
J Med Chem 46: 1429-39 (2003)
Universit£
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.EBI
J Med Chem 46: 1419-28 (2003)
Università
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.EBI
J Med Chem 46: 1408-18 (2003)
Signalgene
Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique.EBI
J Med Chem 46: 1390-407 (2003)
University Of Wuerzburg
Mechanism of action of the diazabicyclononanone-type kappa-agonists.EBI
J Med Chem 46: 1383-9 (2003)
UniversitäT WüRzburg
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.EBI
J Med Chem 46: 1350-8 (2003)
The Danish University Of Pharmaceutical Sciences
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
J Med Chem 46: 1337-49 (2003)
Boehringer Ingelheim Pharmaceuticals
Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor.EBI
J Med Chem 46: 1318-29 (2003)
Università
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.EBI
J Med Chem 46: 1306-17 (2003)
Novo Nordisk
Generation of ligand conformations in continuum solvent consistent with protein active site topology: application to thrombin.EBI
J Med Chem 46: 1293-305 (2003)
Thrombosis Research Institute
Identification of N,N-disubstituted phenylalanines as a novel class of inhibitors of hepatitis C NS5B polymerase.EBI
J Med Chem 46: 1283-5 (2003)
Shire Biochem
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.EBI
J Med Chem 46: 1279-82 (2003)
University Of Maryland
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.BDB
J Am Chem Soc 125: 4087-96 (2003)
Abbott Laboratories
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI
Bioorg Med Chem Lett 13: 1495-8 (2003)
3-Dimensional Pharmaceuticals
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.EBI
Bioorg Med Chem Lett 13: 1487-90 (2003)
Wyeth-Ayerst Research
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.EBI
Bioorg Med Chem Lett 13: 1483-6 (2003)
Glaxosmithkline
Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain.EBI
Bioorg Med Chem Lett 13: 1475-8 (2003)
The Ohio State University
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.EBI
Bioorg Med Chem Lett 13: 1463-7 (2003)
Aventis Pharma Deutschland
From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase.EBI
Bioorg Med Chem Lett 13: 1459-62 (2003)
Centre De Recherche Pierre Fabre
Synthesis and evaluation of a novel series of farnesyl protein transferase inhibitors as non-peptidic CAAX tetrapeptide analogues.EBI
Bioorg Med Chem Lett 13: 1455-8 (2003)
Centre De Recherche Pierre Fabre
Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases.EBI
Bioorg Med Chem Lett 13: 1451-4 (2003)
Oxford University
High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition.EBI
Bioorg Med Chem Lett 13: 1445-9 (2003)
Molecumetics
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.EBI
Bioorg Med Chem Lett 13: 1441-4 (2003)
Merck Research Laboratories
Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.EBI
Bioorg Med Chem Lett 13: 1429-32 (2003)
Universidad Complutense
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.EBI
Bioorg Med Chem Lett 13: 1425-8 (2003)
Pfizer
Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).EBI
Bioorg Med Chem Lett 13: 1415-8 (2003)
Boehringer Ingelheim Pharmaceuticals
Peptoid mimics of agouti related protein.EBI
Bioorg Med Chem Lett 13: 1409-13 (2003)
University Of California
3D-QSAR studies on thieno[3,2-d]pyrimidines as phosphodiesterase IV inhibitors.EBI
Bioorg Med Chem Lett 13: 1403-8 (2003)
National Institute Of Pharmaceutical Education And Research (Niper)
Two new carbazole alkaloids from Murraya koenigii.EBI
J Nat Prod 66: 416-8 (2003)
Chinese Academy Of Sciences
Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.BDB
J Pharmacol Exp Ther 306: 253-61 (2003)
Lcg Bioscience
Synthesis of potent oxindole CDK2 inhibitors.BDB
Bioorg Med Chem 11: 1873-81 (2003)
Hoffmann-La Roche
Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.EBI
Bioorg Med Chem Lett 13: 1385-9 (2003)
Niddk
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.EBI
Bioorg Med Chem Lett 13: 1367-71 (2003)
Abbott Laboratories
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.EBI
Bioorg Med Chem Lett 13: 1363-6 (2003)
Abbott Laboratories
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.BDB
Bioorg Med Chem Lett 13: 1359-62 (2003)
Abbott Laboratories
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.EBI
Bioorg Med Chem Lett 13: 1353-7 (2003)
Merck Research Laboratories
Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.EBI
Bioorg Med Chem Lett 13: 1345-8 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and structure--activity relationships of aroylpyrrole alkylamide bradykinin (B2) antagonists.EBI
Bioorg Med Chem Lett 13: 1341-4 (2003)
Johnson & Johnson Pharmaceutical Research And Development
Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.EBI
Bioorg Med Chem Lett 13: 1337-40 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibition of telomerase by BIBR 1532 and related analogues.EBI
Bioorg Med Chem Lett 13: 1333-6 (2003)
University Of Texas At Dallas
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1325-8 (2003)
Abbott Laboratories
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.EBI
Bioorg Med Chem Lett 13: 1317-20 (2003)
Wyeth Research
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.EBI
Bioorg Med Chem Lett 13: 1313-6 (2003)
Wyeth Research
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.EBI
Bioorg Med Chem Lett 13: 1307-11 (2003)
Roche Research Center
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.EBI
Bioorg Med Chem Lett 13: 1301-5 (2003)
Dainippon Pharmaceutical
Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.EBI
Bioorg Med Chem Lett 13: 1297-300 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.EBI
Bioorg Med Chem Lett 13: 1293-6 (2003)
Abbott Laboratories
[3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.EBI
Bioorg Med Chem Lett 13: 1291-2 (2003)
Pfizer
Phenylacetic acid derivatives as hPPAR agonists.EBI
Bioorg Med Chem Lett 13: 1277-80 (2003)
Merck Research Laboratories
Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.EBI
Bioorg Med Chem Lett 13: 1273-6 (2003)
Bristol-Myers Squibb Pri
Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.EBI
Bioorg Med Chem Lett 13: 1269-72 (2003)
Tohoku Pharmaceutical University
The inhibitory effects of squalene-derived triterpenes on protein phosphatase PP2A.EBI
Bioorg Med Chem Lett 13: 1261-4 (2003)
Instituto Universitario De Bio-Org£Nica
Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand.EBI
Bioorg Med Chem Lett 13: 1241-4 (2003)
Utrecht University
Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors.EBI
Bioorg Med Chem Lett 13: 1231-5 (2003)
Eli Lilly
Interaction of human and rat organic anion transporter 2 with various cephalosporin antibiotics.EBI
Eur J Pharmacol 465: 1-7 (2003)
Kyorin University
Inhibition of P-glycoprotein by newer antidepressants.EBI
J Pharmacol Exp Ther 305: 197-204 (2003)
University Of Heidelberg
Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine.BDB
J Pharmacol Exp Ther 305: 143-50 (2003)
Georgetown University
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.BDB
J Pharmacol Exp Ther 305: 131-42 (2003)
Case Western Reserve University
Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors.BDB
J Pharmacol Exp Ther 305: 57-69 (2003)
Bristol-Myers Squibb Pharmaceuticals Research Institute
Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).BDB
J Pharmacol Exp Ther 305: 1037-44 (2003)
Schering-Plough Research Institute
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.EBI
J Med Chem 46: 1273-6 (2003)
F. Hoffmann-La Roche
2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels.EBI
J Med Chem 46: 1257-65 (2003)
Massachusetts General Hospital
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.EBI
J Med Chem 46: 1229-41 (2003)
Universit£
High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo.EBI
J Med Chem 46: 1220-8 (2003)
Wayne State University
New active series of growth hormone secretagogues.EBI
J Med Chem 46: 1191-203 (2003)
University Of Montpellier
Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives.EBI
J Med Chem 46: 1165-79 (2003)
Link£Ping University
Use of a pharmacophore model to discover a new class of influenza endonuclease inhibitors.EBI
J Med Chem 46: 1153-64 (2003)
Roche Discovery Welwyn
Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors.EBI
J Med Chem 46: 1144-52 (2003)
Universidade Federal Do Rio De Janeiro
Virtual screening for submicromolar leads of tRNA-guanine transglycosylase based on a new unexpected binding mode detected by crystal structure analysis.EBI
J Med Chem 46: 1133-43 (2003)
Philipps-UniversitäT Marburg
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.EBI
J Med Chem 46: 1127-9 (2003)
Université
Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.EBI
J Med Chem 46: 1123-6 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase.EBI
J Med Chem 46: 1120-2 (2003)
Ontogen
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.BDB
J Med Chem 46: 1116-9 (2003)
Sugen
Synthesis and biological evaluation of non-peptidic cyclophilin ligands.EBI
J Med Chem 46: 1112-5 (2003)
Guilford Pharmaceuticals
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents.EBI
J Med Chem 46: 1081-111 (2003)
The Feinberg School Of Medicine Of Northwestern University
Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.EBI
Bioorg Med Chem Lett 13: 1215-9 (2003)
National Cancer Institute-Bethesda
Structure-activity relationships of some opiate glycosides.EBI
Bioorg Med Chem Lett 13: 1207-14 (2003)
Ultrafine Ufc
Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.EBI
Bioorg Med Chem Lett 13: 1203-6 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Indanyl piperazines as melatonergic MT2 selective agents.EBI
Bioorg Med Chem Lett 13: 1199-202 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.EBI
Bioorg Med Chem Lett 13: 1195-8 (2003)
Merck Frosst Centre For Therapeutic Research
N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.EBI
Bioorg Med Chem Lett 13: 1191-4 (2003)
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.EBI
Bioorg Med Chem Lett 13: 1183-6 (2003)
Glaxosmithkline
Interfacial peptide inhibitors of HIV-1 integrase activity and dimerization.EBI
Bioorg Med Chem Lett 13: 1175-7 (2003)
Purdue University
Benzamide derivatives as blockers of Kv1.3 ion channel.EBI
Bioorg Med Chem Lett 13: 1161-4 (2003)
Merck Research Laboratories
Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease.EBI
Bioorg Med Chem Lett 13: 1157-60 (2003)
Bristol-Myers Squibb
Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.EBI
Bioorg Med Chem Lett 13: 1141-5 (2003)
Astrazeneca R&D
Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.EBI
Bioorg Med Chem Lett 13: 1137-9 (2003)
Pfizer
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.BDB
Bioorg Med Chem Lett 13: 1133-6 (2003)
Bristol-Myers Squibb
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.EBI
Bioorg Med Chem Lett 13: 1129-32 (2003)
Merck Frosst Centre For Therapeutic Research
Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors.BDB
Bioorg Med Chem Lett 13: 1115-8 (2003)
Fujisawa Pharmaceutical
Glycine alpha-ketoamides as HCV NS3 protease inhibitors.EBI
Bioorg Med Chem Lett 13: 1111-4 (2003)
Pharmaceutical Research Institute
Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1093-6 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Alkoxysulfamide, N-hydroxysulfamide, and sulfamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.EBI
Bioorg Med Chem Lett 13: 1087-92 (2003)
Seoul National University
Biphenyls as potent vitronectin receptor antagonists. Part 2: biphenylalanine ureas.EBI
Bioorg Med Chem Lett 13: 1071-4 (2003)
Bayer
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.EBI
Bioorg Med Chem Lett 13: 1067-70 (2003)
Glaxosmithkline
Identification of a novel series of selective 5-HT7 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 1055-8 (2003)
Glaxosmithkline
Synthesis and binding affinity of neuropeptide Y at opiate receptors.EBI
Bioorg Med Chem Lett 13: 1029-31 (2003)
University Of North Carolina At Wilmington
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.EBI
Bioorg Med Chem Lett 13: 1023-8 (2003)
Bristol-Myers Squibb
N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship.EBI
Bioorg Med Chem Lett 13: 1015-8 (2003)
Genentech
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.EBI
Bioorg Med Chem Lett 13: 1005-9 (2003)
Universit£
Syntheses and biological properties of cysteine-reactive epibatidine derivatives.EBI
Bioorg Med Chem Lett 13: 1001-4 (2003)
Universit£
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.EBI
Bioorg Med Chem Lett 13: 767-70 (2003)
Bristol-Myers Squibb
Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors.EBI
Bioorg Med Chem Lett 13: 761-5 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 753-6 (2003)
Johnson & Johnson Pharmaceutical Research & Development
1,4-dibenzylpiperazines possess anticocaine activity.EBI
Bioorg Med Chem Lett 13: 749-51 (2003)
University Of Maryland
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors.EBI
Bioorg Med Chem Lett 13: 741-4 (2003)
Merck Frosst Centre For Therapeutic Research
Functional expression and characterization of EryA, the erythritol kinase of Brucella abortus, and enzymatic synthesis of L-erythritol-4-phosphate.EBI
Bioorg Med Chem Lett 13: 737-9 (2003)
Brown University
Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.EBI
Bioorg Med Chem Lett 13: 733-5 (2003)
Virginia Commonwealth University
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.EBI
Bioorg Med Chem Lett 13: 729-32 (2003)
Millennium Pharmaceuticals
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI
Bioorg Med Chem Lett 13: 723-8 (2003)
Millennium Pharmaceuticals
Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase.EBI
Bioorg Med Chem Lett 13: 713-7 (2003)
Merck Research Laboratories
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.EBI
Bioorg Med Chem Lett 13: 709-12 (2003)
Schering-Plough Research Institute
Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist.EBI
Bioorg Med Chem Lett 13: 705-8 (2003)
Schering-Plough Research Institute
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.EBI
Bioorg Med Chem Lett 13: 701-4 (2003)
Neurogen
Orally efficacious NR2B-selective NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 13: 697-700 (2003)
Merck Research Laboratories
Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 13: 693-6 (2003)
Merck Sharp & Dohme Research Laboratories
Exploring new non-sugar sulfated molecules as activators of antithrombin.EBI
Bioorg Med Chem Lett 13: 679-83 (2003)
Virginia Commonwealth University
Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir.EBI
Bioorg Med Chem Lett 13: 669-73 (2003)
Sankyo
Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity.EBI
Bioorg Med Chem Lett 13: 665-8 (2003)
Glaxosmithkline
Design, synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors.EBI
Bioorg Med Chem Lett 13: 657-60 (2003)
Vittal Mallya Scientific Research Foundation
Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution.EBI
Bioorg Med Chem Lett 13: 649-52 (2003)
Roche Research Center
Inhibition of inosine monophosphate dehydrogenase (IMPDH) by 2-[2-(Z)-fluorovinyl]inosine 5'-monophosphate.EBI
Bioorg Med Chem Lett 13: 645-7 (2003)
The University Of Georgia
Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.BDB
Bioorg Med Chem Lett 13: 637-40 (2003)
Glaxosmithkline
Identification of a high-affinity phosphopeptide inhibitor of Stat3.BDB
Bioorg Med Chem Lett 13: 633-6 (2003)
The University Of Texas At Houston
Synthesis of dopamine transporter selective 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes.EBI
Bioorg Med Chem Lett 13: 629-32 (2003)
University Of New Orleans
Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities.EBI
Bioorg Med Chem Lett 13: 609-12 (2003)
Seoul National University
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors.EBI
Bioorg Med Chem Lett 13: 605-8 (2003)
Bristol-Myers Squibb
Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.EBI
Bioorg Med Chem Lett 13: 601-4 (2003)
Seoul National University
Pyridazinones as selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 13: 597-600 (2003)
Merck Frosst Centre For Therapeutic Research
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.EBI
Pharm Res 20: 161-8 (2003)
The University Of Kansas
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.BDB
Neuropsychopharmacology 28: 519-26 (2003)
Case Western Reserve University
Synthesis and pharmacological evaluation of substituted naphth[1,2,3-de]isoquinolines (dinapsoline analogues) as D1 and D2 dopamine receptor ligands.BDB
Bioorg Med Chem 11: 1451-64 (2003)
Purdue University
Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.BDB
J Pharmacol Exp Ther 305: 1104-15 (2003)
University Of Kansas
QSAR and classification of murine and human soluble epoxide hydrolase inhibition by urea-like compounds.EBI
J Med Chem 46: 1066-80 (2003)
The Pennsylvania State University
Systematic development of high affinity bis(ammonio)alkane-type allosteric enhancers of muscarinic ligand binding.EBI
J Med Chem 46: 1031-40 (2003)
University Of W£Rzburg
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.EBI
J Med Chem 46: 1016-30 (2003)
Abbott Laboratories
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.EBI
J Med Chem 46: 954-66 (2003)
University Of Bologna
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.EBI
J Med Chem 46: 925-35 (2003)
Emory University
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.EBI
J Med Chem 46: 921-4 (2003)
Georgetown University Medical Center
Simple, potent, and selective pyrrole inhibitors of monoamine oxidase types A and B.EBI
J Med Chem 46: 917-20 (2003)
Sapienza University Of Rome
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.EBI
J Med Chem 46: 913-6 (2003)
Astrazeneca R&D Charnwood
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions.EBI
J Med Chem 46: 883-908 (2003)
The Feinberg School Of Medicine Of Northwestern University
Modification of the N-terminus of peptidomimetic protein tyrosine phosphatase 1B (PTP1B) inhibitors: identification of analogues with cellular activity.EBI
Bioorg Med Chem Lett 13: 971-5 (2003)
Pharmacia
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.EBI
Bioorg Med Chem Lett 13: 955-9 (2003)
Actelion Pharmaceuticals
Bis-sulfonamides as endothelin receptor antagonists.EBI
Bioorg Med Chem Lett 13: 951-4 (2003)
Actelion Pharmaceuticals
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.EBI
Bioorg Med Chem Lett 13: 931-5 (2003)
Merck Research Laboratories
Acylcyclohexanedione derivatives as potential in vivo sequential inhibitors of 4-hydroxyphenylpyruvate dioxygenase and GA(20) 3beta-hydroxylase.EBI
Bioorg Med Chem Lett 13: 927-30 (2003)
Tunghai University
Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.EBI
Bioorg Med Chem Lett 13: 913-8 (2003)
Kyoto 619-0216
Synthesis of (+),(-)-neamine and their positional isomers as potential antibiotics.EBI
Bioorg Med Chem Lett 13: 901-3 (2003)
Harvard Medical School
Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain.EBI
Bioorg Med Chem Lett 13: 895-9 (2003)
National Cancer Institute-Frederick
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists.EBI
Bioorg Med Chem Lett 13: 885-90 (2003)
Merck Research Laboratories
Design and synthesis of the tumor-activated prodrug of dihydropyrimidine dehydrogenase (DPD) inhibitor, RO0094889 for combination therapy with capecitabine.EBI
Bioorg Med Chem Lett 13: 867-72 (2003)
Nippon Roche Research Center
Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II.EBI
Bioorg Med Chem Lett 13: 863-5 (2003)
University Of Bath
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.EBI
Bioorg Med Chem Lett 13: 851-4 (2003)
Friedrich-Alexander University
Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV.EBI
Bioorg Med Chem Lett 13: 841-5 (2003)
Universit£
Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives.EBI
Bioorg Med Chem Lett 13: 837-40 (2003)
Universit£
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 13: 829-32 (2003)
F. Hoffmann-La Roche
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.EBI
Bioorg Med Chem Lett 13: 817-20 (2003)
Seoul National University
Dehydrophenylalanine derivatives as VLA-4 integrin antagonists.EBI
Bioorg Med Chem Lett 13: 805-8 (2003)
Celltech R&D
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.EBI
Bioorg Med Chem Lett 13: 799-803 (2003)
Tulane University Health Sciences Center
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.EBI
Bioorg Med Chem Lett 13: 795-8 (2003)
Merck Research Laboratories
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.EBI
Bioorg Med Chem Lett 13: 789-94 (2003)
University Of Ljubljana
Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors.EBI
Bioorg Med Chem Lett 13: 785-8 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.EBI
Bioorg Med Chem Lett 13: 783-4 (2003)
University Of Tennessee Health Science Center
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.BDB
Chembiochem 4: 181-5 (2003)
University Of Queensland Brisbane
Exploring sponge-derived terpenoids for their potency and selectivity against 12-human, 15-human, and 15-soybean lipoxygenases.EBI
J Nat Prod 66: 230-5 (2003)
University Of California Santa Cruz
Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1.EBI
Mol Pharmacol 63: 489-98 (2003)
University Of Arizona
Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons.BDB
J Pharmacol Exp Ther 305: 740-8 (2003)
State University Of New York
A tertiary alcohol analog of gamma-hydroxybutyric acid as a specific gamma-hydroxybutyric acid receptor ligand.BDB
J Pharmacol Exp Ther 305: 675-9 (2003)
University Of Maryland
Prolactin releasing peptide has high affinity and efficacy at neuropeptide FF2 receptors.BDB
J Pharmacol Exp Ther 305: 825-32 (2003)
Juvantia Pharma
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.BDB
J Pharmacol Exp Ther 305: 887-96 (2003)
Abbott Laboratories
Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.EBI
J Pharmacol Exp Ther 304: 1161-71 (2003)
Merck Research Laboratories
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.EBI
J Med Chem 46: 876-9 (2003)
Martin-Luther-University Halle-Wittenberg
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI
J Med Chem 46: 868-71 (2003)
Senju Pharmaceutical
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.EBI
J Med Chem 46: 856-67 (2003)
Johannes Gutenberg-University Of Mainz
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.EBI
J Med Chem 46: 838-49 (2003)
Rensselaer Polytechnic Institute
Synthesis and flow cytometric evaluation of novel 1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of nitrobenzylmercaptopurine riboside (NBMPR) designed for probing its conformation when bound to the es nucleoside transporter.EBI
J Med Chem 46: 831-7 (2003)
University Of Tennessee Health Sciences Center
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.EBI
J Med Chem 46: 820-30 (2003)
Methylgene
Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist.EBI
J Med Chem 46: 810-9 (2003)
University Of Arizona
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.EBI
J Med Chem 46: 768-81 (2003)
Università
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes.BDB
J Med Chem 46: 734-46 (2003)
Uppsala University
Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification.EBI
J Med Chem 46: 716-26 (2003)
University Of Innsbruck
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.EBI
J Med Chem 46: 702-15 (2003)
Dainippon Pharmaceutical
Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor.EBI
J Med Chem 46: 691-701 (2003)
Sumitomo Pharmaceuticals
Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.BDB
J Med Chem 46: 685-90 (2003)
Aventis Pharma
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.EBI
J Med Chem 46: 681-4 (2003)
Aventis Pharmaceuticals
2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists.EBI
J Med Chem 46: 677-80 (2003)
Harvard University
Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases.EBI
J Med Chem 46: 674-6 (2003)
Enanta Pharmaceuticals
In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.EBI
J Med Chem 46: 670-3 (2003)
Pfizer
Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists.EBI
J Med Chem 46: 666-9 (2003)
Tsukuba Research Institute
Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation.BDB
Chem Biol 10: 15-24 (2003)
Tohoku University
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.EBI
J Med Chem 46: 646-9 (2003)
Università
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity.EBI
J Med Chem 46: 642-5 (2003)
National Institute On Drug Abuse
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.EBI
J Med Chem 46: 623-33 (2003)
Glaxosmithkline
Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.EBI
J Med Chem 46: 601-8 (2003)
Columbia University
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and as potential antitumor agents.EBI
J Med Chem 46: 591-600 (2003)
Duquesne University
Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity.EBI
J Med Chem 46: 584-90 (2003)
University Centre For Pharmacy
Design, synthesis, and biological evaluation of a series of fluoroquinoanthroxazines with contrasting dual mechanisms of action against topoisomerase II and G-quadruplexes.EBI
J Med Chem 46: 571-83 (2003)
The University Of Arizona
Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.EBI
J Med Chem 46: 542-57 (2003)
Universit£
Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5.EBI
J Med Chem 46: 486-98 (2003)
Aventis Pharma Deutschland
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.EBI
J Med Chem 46: 461-73 (2003)
Merck Research Laboratories
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.EBI
J Med Chem 46: 457-60 (2003)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.EBI
J Med Chem 46: 453-6 (2003)
Merck Research Laboratories
Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors.BDB
Fundam Clin Pharmacol 16: 317-23 (2002)
Shinshu University
Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.EBI
Anticancer Drugs 14: 175-81 (2003)
Korea Research Institute Of Chemical Technology
Condensed aromatic peptide family of microbial metabolites, inhibitors of CD28-CD80 interactions.EBI
Bioorg Med Chem Lett 13: 573-5 (2003)
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.EBI
Bioorg Med Chem Lett 13: 567-71 (2003)
Schering-Plough Research Institute
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.EBI
Bioorg Med Chem Lett 13: 561-6 (2003)
Millennium Pharmaceuticals
Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.EBI
Bioorg Med Chem Lett 13: 553-6 (2003)
National Institute Of Diabetes And Digestive And Kidney Diseases
Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.EBI
Bioorg Med Chem Lett 13: 547-51 (2003)
Bristol-Myers Squibb Pri
Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.EBI
Bioorg Med Chem Lett 13: 543-6 (2003)
Bristol-Myers Squibb Pri
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.EBI
Bioorg Med Chem Lett 13: 533-8 (2003)
Bristol-Myers Squibb Pharmaceuticals
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.EBI
Bioorg Med Chem Lett 13: 529-32 (2003)
Southern Research Institute
5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors.EBI
Bioorg Med Chem Lett 13: 525-7 (2003)
University Of California
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors.EBI
Bioorg Med Chem Lett 13: 513-7 (2003)
University Of Michigan
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.EBI
Bioorg Med Chem Lett 13: 507-11 (2003)
Berlex Biosciences
Thiophene-based vitronectin receptor antagonists.EBI
Bioorg Med Chem Lett 13: 503-6 (2003)
Shire Biochem
1,4-Diazepane-2-ones as novel inhibitors of LFA-1.EBI
Bioorg Med Chem Lett 13: 499-502 (2003)
Novartis Institute For Biomedical Research
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).EBI
Bioorg Med Chem Lett 13: 479-83 (2003)
Merck Research Laboratories
p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.EBI
Bioorg Med Chem Lett 13: 467-70 (2003)
Merck
Modelling of carbonic anhydrase inhibitory activity of sulfonamides using molecular negentropy.EBI
Bioorg Med Chem Lett 13: 447-53 (2003)
A.P.S. University
Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.EBI
Bioorg Med Chem Lett 13: 443-6 (2003)
Università
Discovery of orally bioavailable NK1 receptor antagonists.EBI
Bioorg Med Chem Lett 13: 437-42 (2003)
Ucb Pharma
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.EBI
Bioorg Med Chem Lett 13: 427-31 (2003)
Merck Research Laboratories
A series of 2(Z)-2-benzylidene-6,7-dihydroxybenzofuran-3[2H]-ones as inhibitors of chorismate synthase.EBI
Bioorg Med Chem Lett 13: 423-6 (2003)
Pantherix
2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 13: 413-7 (2003)
Amorepacific
SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.EBI
Bioorg Med Chem Lett 13: 405-8 (2003)
Solvay Pharma
Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.EBI
Bioorg Med Chem Lett 13: 387-9 (2003)
The Oxford Centre For Molecular Sciences And The Dyson Perrins Laboratory
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.EBI
Bioorg Med Chem Lett 13: 379-82 (2003)
Pfizer
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.EBI
Bioorg Med Chem Lett 13: 369-73 (2003)
Bristol-Myers Squibb
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.EBI
Bioorg Med Chem Lett 13: 351-4 (2003)
Merck Research Laboratories
Imidazopyrimidines, potent inhibitors of p38 MAP kinase.EBI
Bioorg Med Chem Lett 13: 347-50 (2003)
Johnson & Johnson Pharmaceutical Research And Development
Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors.EBI
Bioorg Med Chem Lett 13: 331-4 (2003)
Leiden University
AF2 interaction with Ascaris suum body wall muscle membranes involves G-protein activation.BDB
Biochem Biophys Res Commun 301: 456-9 (2003)
Pharmacia
Cationic reduction of bastadin-4 to bastadin-5. Preparation of 5-[2h]-bastadin-5 by site-specific isotopic labeling.EBI
J Nat Prod 66: 112-4 (2003)
University Of California
Chemical and biological investigation of the fungus Pulveroboletus ravenelii.EBI
J Nat Prod 66: 103-7 (2003)
The University Of Mississippi
Flavanone glycosides from Miconia trailii.EBI
J Nat Prod 66: 39-41 (2003)
University Of Mississippi
Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction.EBI
J Med Chem 46: 441-4 (2003)
Johnson & Johnson Pharmaceutical Research & Development
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.EBI
J Med Chem 46: 417-26 (2003)
Aristotle University Of Thessaloniki
Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity.EBI
J Med Chem 46: 399-408 (2003)
Glaxosmithkline
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.EBI
J Med Chem 46: 364-73 (2003)
Georgetown University Medical Center
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.EBI
J Med Chem 46: 353-5 (2003)
Pfizer
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.EBI
J Med Chem 46: 349-52 (2003)
Merck Research Laboratories
Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.EBI
J Med Chem 46: 345-8 (2003)
Mrl Rome
5-HT4 receptor ligands: applications and new prospects.EBI
J Med Chem 46: 319-44 (2003)
Paris-Sud University
Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species.BDB
Protein Sci 12: 349-60 (2003)
Gsk
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.BDB
J Pharmacol Exp Ther 304: 818-26 (2003)
Taisho Pharmaceutical
Agmatine is efficiently transported by non-neuronal monoamine transporters extraneuronal monoamine transporter (EMT) and organic cation transporter 2 (OCT2).EBI
J Pharmacol Exp Ther 304: 810-7 (2003)
University Of Cologne
Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A.EBI
J Pharmacol Exp Ther 304: 610-6 (2003)
Kitasato University
Interaction of cysteine conjugates with human and rabbit organic anion transporter 1.EBI
J Pharmacol Exp Ther 304: 560-6 (2003)
University Of Arizona
The specificities of protein kinase inhibitors: an update.BDB
Biochem J 371: 199-204 (2003)
University Of Dundee
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.BDB
Biochemistry 42: 631-8 (2003)
The Johns Hopkins University
Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists.EBI
Mol Cancer Ther 2: 105-12 (2003)
Japanese Foundation For Cancer Research
Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.BDB
Biochem Pharmacol 65: 435-40 (2003)
Aventis Pharma
Prodrugs of purine and pyrimidine analogues for the intestinal di/tri-peptide transporter PepT1: affinity for hPepT1 in Caco-2 cells, drug release in aqueous media and in vitro metabolism.EBI
J Control Release 86: 279-92 (2003)
The Royal Danish School Of Pharmacy
Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4).EBI
Biochem J 371: 361-7 (2003)
The Netherlands Cancer Institute
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.EBI
J Med Chem 46: 314-7 (2003)
University Of Bath
Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.EBI
J Med Chem 46: 310-3 (2003)
University Of Firenze
Discovery of a long-chain carbamoyl aminocarnitine derivative, a reversible carnitine palmitoyltransferase inhibitor with antiketotic and antidiabetic activity.EBI
J Med Chem 46: 303-9 (2003)
Sigma Tau Pharmaceutical Industries
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.EBI
J Med Chem 46: 265-83 (2003)
H. Lundbeck
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.EBI
J Med Chem 46: 255-64 (2003)
F. Hoffmann-La Roche
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.EBI
J Med Chem 46: 244-54 (2003)
National Cancer Institute-Frederick
Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.EBI
J Med Chem 46: 237-43 (2003)
University Of Pennsylvania
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.BDB
J Med Chem 46: 222-36 (2003)
Faculte De Medecine Et De Pharmacie
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.EBI
J Med Chem 46: 210-3 (2003)
Pfizer
Potential tumor-selective nitroimidazolylmethyluracil prodrug derivatives: inhibitors of the angiogenic enzyme thymidine phosphorylase.EBI
J Med Chem 46: 207-9 (2003)
University Of Manchester
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.EBI
J Med Chem 46: 204-6 (2003)
Merck Research Laboratories
Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity.BDB
J Am Chem Soc 125: 363-73 (2003)
Weizmann Institute Of Science
Activity of opioid ligands in cells expressing cloned mu opioid receptors.BDB
BMC Pharmacol 3: 1 (2003)
Molecular Research Institute
New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor.EBI
J Med Chem 46: 161-8 (2002)
Universit£
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.EBI
J Med Chem 46: 155-60 (2002)
Industrial Research
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.EBI
J Med Chem 46: 138-47 (2002)
Université
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.EBI
J Med Chem 46: 125-37 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.EBI
J Med Chem 46: 113-24 (2002)
Takeda Chemical Industries
Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence.EBI
J Med Chem 46: 105-12 (2002)
Kissei Pharmaceutical
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.EBI
J Med Chem 46: 74-86 (2002)
Vrije Universiteit
Hydantoin-substituted 4,6-dichloroindole-2-carboxylic acids as ligands with high affinity for the glycine binding site of the NMDA receptor.EBI
J Med Chem 46: 64-73 (2002)
Johannes Gutenberg-UniversitäT
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).EBI
J Med Chem 46: 49-63 (2002)
Wyeth Research
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.EBI
J Med Chem 46: 34-48 (2002)
Universit£
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.EBI
J Med Chem 46: 9-11 (2002)
Amgen
Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.EBI
J Med Chem 46: 1-4 (2002)
Universit£
Sodium 1-(12-hydroxy)octadecanyl sulfate, an MMP2 inhibitor, isolated from a tunicate of the family Polyclinidae.EBI
J Nat Prod 65: 1936-8 (2002)
The University Of Tokyo
New polyhydroxylated pyrrolidine, piperidine, and pyrrolizidine alkaloids from Scilla sibirica.EBI
J Nat Prod 65: 1875-81 (2002)
Hokuriku University
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.EBI
J Nat Prod 65: 1749-53 (2002)
Université
Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition.BDB
Chem Biol 9: 1323-8 (2002)
Massachusetts Institute Of Technology
Synthesis and evaluation of phosphoramidate amino acid-based inhibitors of sialyltransferases.EBI
Bioorg Med Chem Lett 13: 301-4 (2002)
University Of Colorado
Design and synthesis of factor Xa inhibitors and their prodrugs.EBI
Bioorg Med Chem Lett 13: 297-300 (2002)
Millennium Pharmaceuticals
CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine.EBI
Bioorg Med Chem Lett 13: 289-91 (2003)
Bristol-Myers Squibb
Development of a presynaptic 5-HT1A antagonist.EBI
Bioorg Med Chem Lett 13: 285-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI
Bioorg Med Chem Lett 13: 277-80 (2002)
Merck Research Laboratories
p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.EBI
Bioorg Med Chem Lett 13: 273-6 (2003)
Merck Research Laboratories
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists.EBI
Bioorg Med Chem Lett 13: 269-71 (2003)
Pfizer
Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.EBI
Bioorg Med Chem Lett 13: 261-4 (2002)
Ligand Pharmaceuticals
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.EBI
Bioorg Med Chem Lett 13: 257-60 (2002)
Novo Nordisk
Synthesis of non-competitive inhibitors of sphingomyelinases with significant activity.EBI
Bioorg Med Chem Lett 13: 229-36 (2002)
Tokyo University Of Pharmacy & Life Science
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.BDB
Bioorg Med Chem Lett 13: 217-22 (2003)
University Of Newcastle
Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties.EBI
Bioorg Med Chem Lett 13: 209-12 (2002)
Institut Henri Beaufour
[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).EBI
Bioorg Med Chem Lett 13: 201-4 (2002)
National Institute Of Radiological Sciences
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.EBI
Bioorg Med Chem Lett 13: 175-8 (2002)
University Of Santiago
alpha1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus.EBI
Bioorg Med Chem Lett 13: 171-3 (2002)
Università
Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones.EBI
Bioorg Med Chem Lett 13: 165-9 (2002)
Basf
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.EBI
Bioorg Med Chem Lett 13: 161-4 (2002)
Merck Research Laboratories
Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide.EBI
J Med Chem 45: 5755-75 (2002)
Novo Nordisk
Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors.EBI
J Med Chem 45: 5745-54 (2002)
The Royal Danish School Of Pharmacy
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.EBI
J Med Chem 45: 5736-44 (2002)
University Of Florida
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.EBI
J Med Chem 45: 5727-35 (2002)
Universit£
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.EBI
J Med Chem 45: 5710-20 (2002)
Università
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.EBI
J Med Chem 45: 5687-93 (2002)
Novartis Pharma
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).EBI
J Med Chem 45: 5671-86 (2002)
Bulgarian Academy Of Sciences
Metal-dependent inhibition of HIV-1 integrase.EBI
J Med Chem 45: 5661-70 (2002)
University Of Southern California
In silico and NMR identification of inhibitors of the IGF-I and IGF-binding protein-5 interaction.EBI
J Med Chem 45: 5655-60 (2002)
Institute For Biochemistry
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.EBI
J Med Chem 45: 5640-8 (2002)
Merck Research Laboratories
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.EBI
J Med Chem 45: 5628-39 (2002)
Abbott Laboratories
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.EBI
J Med Chem 45: 5617-9 (2002)
University Of Maryland
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.EBI
J Med Chem 45: 5609-16 (2002)
Merck Research Laboratories
Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor.EBI
Biochemistry 41: 14916-14924 (2002)
Ucla And The Wadsworth Veterans Administration Hospital
Urate transport via human PAH transporter hOAT1 and its gene structure.EBI
Kidney Int 63: 143-55 (2003)
Jikei University School Of Medicine
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.EBI
Bioorg Med Chem Lett 13: 139-41 (2002)
Currently Naeja Pharmaceutical
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.EBI
Bioorg Med Chem Lett 13: 133-7 (2002)
Roche Research Center
Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.EBI
Bioorg Med Chem Lett 13: 129-31 (2003)
Bristol-Myers Squibb
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.EBI
Bioorg Med Chem Lett 13: 125-8 (2003)
Bristol-Myers Squibb
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.EBI
Bioorg Med Chem Lett 13: 119-23 (2002)
Merck Research Laboratories
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.EBI
Bioorg Med Chem Lett 13: 111-3 (2002)
Banyu Tsukuba Research Institute
Design of novel N-(2,4-dioxo-1,2,3,4-tetrahydro-thieno[3,2-d]pyrimidin-7-yl)-guanidines as thymidine phosphorylase inhibitors, and flexible docking to a homology model.EBI
Bioorg Med Chem Lett 13: 107-10 (2002)
Attenuon
N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors.EBI
Bioorg Med Chem Lett 13: 97-100 (2002)
Chinese Academy Of Sciences
Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere.EBI
Bioorg Med Chem Lett 13: 93-6 (2002)
Kyoto Pharmaceutical University
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3.EBI
Bioorg Med Chem Lett 13: 87-91 (2003)
Nippon Roche Research Center
Fluorescent bioprobes for visualization of puromycin-sensitive aminopeptidase in living cells.EBI
Bioorg Med Chem Lett 13: 83-6 (2002)
The University Of Tokyo
Rational approaches towards reversible inhibition of type B monoamine oxidase. Design and evaluation of a novel 5H-Indeno[1,2-c]pyridazin-5-one derivative.EBI
Bioorg Med Chem Lett 13: 69-73 (2002)
FacultéS Universitaires Notre-Dame De La Paix
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.EBI
Bioorg Med Chem Lett 13: 61-4 (2003)
Meiji Seika Kaisha
Homologues and isomers of noladin ether, a putative novel endocannabinoid: interaction with rat cannabinoid CB(1) receptors.EBI
Bioorg Med Chem Lett 13: 43-6 (2002)
Discaff
Synthesis and gamma-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres.EBI
Bioorg Med Chem Lett 13: 37-41 (2002)
Merck Sharp & Dohme Research Laboratories
Identification of a stable chymase inhibitor using a pharmacophore-Based database search.EBI
Bioorg Med Chem Lett 13: 25-9 (2002)
Toa Eiyo
Etoricoxib.BDB
Drugs 62: 2637 (2002)
Adis International
Hybrid ubiquinone: novel inhibitor of mitochondrial complex I.EBI
Biochim Biophys Acta 1556: 106-12 (2002)
Kyoto University
Use of ab initio calculations to predict the biological potency of carboxylesterase inhibitors.EBI
J Med Chem 45: 5576-93 (2002)
University Of California
Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 1.EBI
J Med Chem 45: 5564-75 (2002)
Dainippon Pharmaceutical
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.EBI
J Med Chem 45: 5556-63 (2002)
University Of Cagliari
Crystal structures of dipeptides containing the Dmt-Tic pharmacophore.EBI
J Med Chem 45: 5506-13 (2002)
National Institute Of Environmental Health Sciences
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.EBI
J Med Chem 45: 5492-505 (2002)
Glaxosmithkline
Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors.EBI
J Med Chem 45: 5471-82 (2002)
Boehringer Ingelheim Pharmaceuticals
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.EBI
J Med Chem 45: 5430-9 (2002)
Uppsala University
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.EBI
J Med Chem 45: 5415-8 (2002)
Schering-Plough Research Institute
Total synthesis and biological evaluation of (5Z,9Z)-5,9-hexadecadienoic acid, an inhibitor of human topoisomerase I.EBI
J Nat Prod 65: 1715-8 (2002)
University Of Puerto Rico
Aldehyde dehydrogenase inhibitors from the mushroom Clitocybe clavipes.EBI
J Nat Prod 65: 1712-4 (2002)
Shizuoka University
Triterpenoid constituents isolated from the bark of Abies sachalinensis.EBI
J Nat Prod 65: 1657-9 (2002)
Osaka University Of Pharmaceutical Sciences
Antioxidant and free-radical scavenging activity of constituents of the leaves of Tachigalia paniculata.EBI
J Nat Prod 65: 1526-9 (2002)
Università
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.EBI
J Nat Prod 65: 1517-21 (2002)
Uppsala University
Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3635-9 (2002)
Agouron Pharmaceuticals
Inhibition of amine oxidases activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives.EBI
Bioorg Med Chem Lett 12: 3629-33 (2002)
Sapienza University Of Rome
Silanediol-based inhibitor of thermolysin.EBI
Bioorg Med Chem Lett 12: 3625-7 (2002)
State University Of New York
Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter.EBI
Bioorg Med Chem Lett 12: 3611-3 (2002)
Institutet
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.EBI
Bioorg Med Chem Lett 12: 3601-4 (2002)
Université
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the metal binding group.EBI
Bioorg Med Chem Lett 12: 3595-9 (2002)
British Biotech Pharmaceuticals
Novel 1',1'-chain substituted Delta(8)-tetrahydrocannabinols.EBI
Bioorg Med Chem Lett 12: 3583-6 (2002)
National Hellenic Research Foundation
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI
Bioorg Med Chem Lett 12: 3573-7 (2002)
Janssen-Cilag
Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators.EBI
Bioorg Med Chem Lett 12: 3565-7 (2002)
Biovitrum
Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.EBI
Bioorg Med Chem Lett 12: 3551-5 (2002)
University Of Bari
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.BDB
Bioorg Med Chem Lett 12: 3537-41 (2002)
Merck Research Laboratories
SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization.BDB
J Pharmacol Exp Ther 303: 1171-9 (2002)
Sanofi-SynthÉLabo Recherche
Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin.BDB
J Pharmacol Exp Ther 303: 1052-60 (2002)
Merck Sharp And Dohme Research Laboratories
[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.BDB
J Pharmacol Exp Ther 303: 1044-51 (2002)
Merck Research Laboratories
The cation transporters rOCT1 and rOCT2 interact with bicarbonate but play only a minor role for amantadine uptake into rat renal proximal tubules.EBI
J Pharmacol Exp Ther 303: 959-68 (2002)
University Of Manitoba
Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.BDB
Neuropsychopharmacology 27: 699-711 (2002)
Eli Lilly
Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.EBI
J Med Chem 45: 5410-3 (2002)
Università
Adenosine 5'-O-(1-boranotriphosphate) derivatives as novel P2Y(1) receptor agonists.EBI
J Med Chem 45: 5384-96 (2002)
Bar-Ilan University
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.EBI
J Med Chem 45: 5378-83 (2002)
University Of Innsbruck
Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes.EBI
J Med Chem 45: 5358-64 (2002)
Free University Of Berlin
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.EBI
J Med Chem 45: 5353-7 (2002)
Universit£
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.EBI
J Med Chem 45: 5321-9 (2002)
National Research Council Of Canada
Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles.EBI
J Med Chem 45: 5303-10 (2002)
Johnson & Johnson Pharmaceutical Research & Development
Sulfamide-based inhibitors for carboxypeptidase A. Novel type transition state analogue inhibitors for zinc proteases.EBI
J Med Chem 45: 5295-302 (2002)
Pohang University Of Science And Technology
Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.EBI
J Med Chem 45: 5287-94 (2002)
University Of Arizona
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.EBI
J Med Chem 45: 5280-6 (2002)
Purdue Pharma
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.BDB
J Med Chem 45: 5260-79 (2002)
Teva Pharmaceutical Industries
Molecular docking and 3D-QSAR studies on gag peptide analogue inhibitors interacting with human cyclophilin A.EBI
J Med Chem 45: 5249-59 (2002)
Chinese Academy Of Sciences
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).BDB
J Med Chem 45: 5233-48 (2002)
Bristol-Myers Squibb
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.BDB
J Med Chem 45: 5224-32 (2002)
Bristol-Myers Squibb
Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight.BDB
J Biol Chem 278: 1831-6 (2003)
University Of Padova
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3491-5 (2002)
Neurocrine Biosciences
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.EBI
Bioorg Med Chem Lett 12: 3487-90 (2002)
Wyeth Research
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.EBI
Bioorg Med Chem Lett 12: 3483-6 (2002)
Merck Research Laboratories
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.EBI
Bioorg Med Chem Lett 12: 3479-82 (2002)
Schering-Plough Research Institute
Synthesis of [difluoro-(3-alkenylphenyl)-methyl]-phosphonic acids on non-crosslinked polystyrene and their evaluation as inhibitors of PTP1B.EBI
Bioorg Med Chem Lett 12: 3471-4 (2002)
University Of Waterloo
The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3467-70 (2002)
Agouron Pharmaceuticals
Six-membered cyclic ureas as HIV-1 protease inhibitors: a QSAR study based on CODESSA PRO approach. Quantitative structure-activity relationships.EBI
Bioorg Med Chem Lett 12: 3453-7 (2002)
University Of Florida
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.EBI
Bioorg Med Chem Lett 12: 3449-52 (2002)
Glaxosmithkline
Trifluoromethyl ketones as inhibitors of histone deacetylase.EBI
Bioorg Med Chem Lett 12: 3443-7 (2002)
Abbott Laboratories
Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease.BDB
Bioorg Med Chem Lett 12: 3431-3 (2002)
Glaxosmithkline
Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3421-4 (2002)
Bayer Research Center
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.EBI
Bioorg Med Chem Lett 12: 3417-9 (2002)
Currently Naeja Pharmaceutical
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.EBI
Bioorg Med Chem Lett 12: 3413-5 (2002)
Currently Naeja Pharmaceutical
Natural PTP1B inhibitors from Broussonetia papyrifera.EBI
Bioorg Med Chem Lett 12: 3387-90 (2002)
Chinese Academy Of Sciences
Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.EBI
Bioorg Med Chem Lett 12: 3383-6 (2002)
Pharmacia
Chemical modification of reveromycin A and its biological activities.EBI
Bioorg Med Chem Lett 12: 3363-6 (2002)
Riken (The Institute Of Physical And Chemical Research)
Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.EBI
Bioorg Med Chem Lett 12: 3359-62 (2002)
Glaxosmithkline
Spectral and crystallographic study of pyridinic analogues of nimesulide: determination of the active form of methanesulfonamides as COX-2 selective inhibitors.EBI
J Med Chem 45: 5182-5 (2002)
Université
Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.EBI
J Med Chem 45: 5173-81 (2002)
Duquesne University
Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging.EBI
J Med Chem 45: 5150-6 (2002)
Forschungszentrum JüLich
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.EBI
J Med Chem 45: 5136-49 (2002)
University Of LièGe
Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB).EBI
J Med Chem 45: 5081-9 (2002)
Daiichi Fine Chemical
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.EBI
J Med Chem 45: 5043-51 (2002)
Neurogen
Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists.EBI
J Med Chem 45: 5030-6 (2002)
Università
Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.BDB
J Med Chem 45: 5005-22 (2002)
Sunesis Pharmaceuticals
Thrombin inhibition by novel benzamidine derivatives: a free-energy perturbation study.EBI
J Med Chem 45: 4995-5004 (2002)
Universidade Federal Do Rio De Janeiro
Synthesis, solution structure, and biological evaluation of urokinase type plasminogen activator (uPA)-derived receptor binding domain mimetics.EBI
J Med Chem 45: 4984-94 (2002)
Technische UniversitäT MüNchen
Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum.EBI
J Med Chem 45: 4975-83 (2002)
The University Of Liverpool
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.EBI
J Med Chem 45: 4961-74 (2002)
Pfizer
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.EBI
J Med Chem 45: 4954-7 (2002)
Bristol-Myers Squibb
Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).EBI
J Med Chem 45: 4950-3 (2002)
Acadia Pharmaceuticals
The human bile salt export pump: characterization of substrate specificity and identification of inhibitors.EBI
Gastroenterology 123: 1649-58 (2002)
King'S College Hospital
Crystal structures of Candida albicans N-myristoyltransferase with two distinct inhibitors.BDB
Chem Biol 9: 1119-28 (2002)
Nippon Roche Research Center
Panepophenanthrin, from a mushroom strain, a novel inhibitor of the ubiquitin-activating enzyme.EBI
J Nat Prod 65: 1491-3 (2002)
Institute Of Microbial Chemistry
Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors.EBI
J Nat Prod 65: 1479-85 (2002)
University Of Bonn
Constituents of the stigmas of Crocus sativus and their tyrosinase inhibitory activity.EBI
J Nat Prod 65: 1452-6 (2002)
National Cheng Kung University
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.EBI
Bioorg Med Chem Lett 12: 3341-4 (2002)
Glaxosmithkline
3-Hydroxy-4-methyl-5-pentyl-2-iminopyrrolidine: a potent and highly selective inducible nitric oxide synthase inhibitor.EBI
Bioorg Med Chem Lett 12: 3337-9 (2002)
Pharmacia
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3329-32 (2002)
Merck Research Laboratories
Capped dipeptide alpha-ketoacid inhibitors of the HCV NS3 protease.EBI
Bioorg Med Chem Lett 12: 3325-8 (2002)
Irbm, Mrl Rome
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.EBI
Bioorg Med Chem Lett 12: 3317-20 (2002)
Merck Frosst Centre For Therapeutic Research
Novel human histamine H(3) receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3309-12 (2002)
Johnson And Johnson Pharmaceutical Research And Development
The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors.EBI
Bioorg Med Chem Lett 12: 3305-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.EBI
Bioorg Med Chem Lett 12: 3291-6 (2002)
Institut De Recherches Servier
Identification of novel inhibitors of fibroblast growth factor (FGF-2) binding to heparin and endothelial cell survival from a structurally diverse carbohybrid library.EBI
Bioorg Med Chem Lett 12: 3287-90 (2002)
University College Dublin
Synthesis and biological activity of olomoucine II.EBI
Bioorg Med Chem Lett 12: 3283-6 (2002)
Palack£
Discovery and biological characterization of capromorelin analogues with extended half-lives.EBI
Bioorg Med Chem Lett 12: 3279-82 (2002)
Pfizer
Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.EBI
Bioorg Med Chem Lett 12: 3271-3 (2002)
Kyorin Pharmaceutical
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.BDB
J Pharmacol Exp Ther 303: 791-804 (2002)
Institut De Recherches Servier
Elucidation of the vasoactive intestinal peptide pharmacophore for VPAC(2) receptors in human and rat and comparison to the pharmacophore for VPAC(1) receptors.BDB
J Pharmacol Exp Ther 303: 445-60 (2002)
Nih
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.EBI
J Med Chem 45: 4923-30 (2002)
Pharmazeutisches Institut Der Universit£T Freiburg
Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide.EBI
J Med Chem 45: 4913-22 (2002)
Eisai
Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.EBI
J Med Chem 45: 4875-87 (2002)
Universit£
Computer-aided design of selective COX-2 inhibitors: comparative molecular field analysis, comparative molecular similarity indices analysis, and docking studies of some 1,2-diarylimidazole derivatives.EBI
J Med Chem 45: 4847-57 (2002)
University Of Hyderabad
Kappa-opioid receptor model in a phospholipid bilayer: molecular dynamics simulation.EBI
J Med Chem 45: 4838-46 (2002)
University Of Catania
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.EBI
J Med Chem 45: 4816-27 (2002)
Chinese Academy Of Sciences
Benzimidazole derivatives. 3. 3D-QSAR/CoMFA model and computational simulation for the recognition of 5-HT(4) receptor antagonists.EBI
J Med Chem 45: 4806-15 (2002)
Universidad Complutense
Synthesis of potent and highly selective inhibitors of human tryptase.EBI
Bioorg Med Chem Lett 12: 3235-8 (2002)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI
Bioorg Med Chem Lett 12: 3229-33 (2002)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.EBI
Bioorg Med Chem Lett 12: 3219-22 (2002)
Glaxosmithkline
Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.EBI
Bioorg Med Chem Lett 12: 3203-5 (2002)
Schering-Plough Research Institute
P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.EBI
Bioorg Med Chem Lett 12: 3199-202 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.EBI
Bioorg Med Chem Lett 12: 3195-8 (2002)
Ucb Pharma
Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.EBI
Bioorg Med Chem Lett 12: 3191-3 (2002)
Daiichi Pharmaceutical
Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI
Bioorg Med Chem Lett 12: 3187-90 (2002)
Bayer
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.EBI
Bioorg Med Chem Lett 12: 3183-6 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
New irreversible adenosine A(1) antagonists based on FSCPX.EBI
Bioorg Med Chem Lett 12: 3179-82 (2002)
Monash University (Parkville Campus)
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.EBI
Bioorg Med Chem Lett 12: 3175-8 (2002)
Institute For Molecular Studies
A mechanism-based probe for gp120-Hydrolyzing antibodies.EBI
Bioorg Med Chem Lett 12: 3167-70 (2002)
University Of Texas-Houston Medical School
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.EBI
Bioorg Med Chem Lett 12: 3161-5 (2002)
Schering-Plough Research Institute
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.EBI
Bioorg Med Chem Lett 12: 3157-60 (2002)
Schering-Plough Research Institute
Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.EBI
Bioorg Med Chem Lett 12: 3153-6 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.EBI
Bioorg Med Chem Lett 12: 3149-52 (2002)
Schering-Plough Research Institute
Synthesis and biological activity of retinoic acid receptor-alpha specific amides.EBI
Bioorg Med Chem Lett 12: 3145-8 (2002)
Allergan
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.EBI
Bioorg Med Chem Lett 12: 3141-3 (2002)
Shire Biochem
Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease.EBI
Bioorg Med Chem Lett 12: 3129-33 (2002)
Celera
A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.EBI
Bioorg Med Chem Lett 12: 3125-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.EBI
Bioorg Med Chem Lett 12: 3111-5 (2002)
Neurogen
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.EBI
Bioorg Med Chem Lett 12: 3105-9 (2002)
Neurogen
Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives.EBI
Bioorg Med Chem Lett 12: 3097-9 (2002)
Egis Pharmaceuticals
Hydroxamate based inhibitors of adenylyl cyclase. Part 2: the effect of cyclic linkers on P-site binding.EBI
Bioorg Med Chem Lett 12: 3089-92 (2002)
Millennium Pharmaceuticals
Hydroxamate based inhibitors of adenylyl cyclase. Part 1: the effect of acyclic linkers on P-site binding.EBI
Bioorg Med Chem Lett 12: 3085-8 (2002)
Millennium Pharmaceuticals
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.EBI
Bioorg Med Chem Lett 12: 3081-4 (2002)
Johnson And Johnson Pharmaceutical Research And Development
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.EBI
Bioorg Med Chem Lett 12: 3077-9 (2002)
Abbott Laboratories
Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands.EBI
Bioorg Med Chem Lett 12: 3073-6 (2002)
F. Hoffmann-La Roche
bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors.EBI
Bioorg Med Chem Lett 12: 3067-71 (2002)
University Of Kentucky
Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1.EBI
Bioorg Med Chem Lett 12: 3059-62 (2002)
Novartis Institute For Biomedical Research
Synthesis and evaluation of potent pyrrolidine H(3) antagonists.EBI
Bioorg Med Chem Lett 12: 3055-8 (2002)
Abbott Laboratories
alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: structure-Activity relationship.EBI
Bioorg Med Chem Lett 12: 3047-50 (2002)
The Ohio State University
Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.EBI
Bioorg Med Chem Lett 12: 3041-5 (2002)
Tsukuba Research Institute
Solvent and guest isotope effects on complexation thermodynamics of alpha-, beta-, and 6-amino-6-deoxy-beta-cyclodextrins.BDB
J Am Chem Soc 124: 12361-71 (2002)
Japan Science And Technology Agency
2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study.BDB
J Enzyme Inhib Med Chem 17: 45-8 (2002)
University Of Porto-Rua Anibal Cunha
Synthesis and structure-activity relationship of the isoindolinyl benzisoxazolpiperidines as potent, selective, and orally active human dopamine D4 receptor antagonists.BDB
Chembiochem 3: 999-1009 (2002)
Aventis Pharmaceuticals
Comparison of 3D structures and AT(1) binding properties of pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones with parent antihypertensive drug irbesartan.EBI
J Med Chem 45: 4794-8 (2002)
Université
Synthesis and investigation of conformationally restricted analogues of lavendustin A as cytotoxic inhibitors of tubulin polymerization.EBI
J Med Chem 45: 4774-85 (2002)
Purdue University
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues.EBI
J Med Chem 45: 4755-61 (2002)
Research Triangle Institute
The effect of exchanging various substituents at the 2-position of 2-methoxyestradiol on cytotoxicity in human cancer cell cultures and inhibition of tubulin polymerization.EBI
J Med Chem 45: 4748-54 (2002)
Purdue University
Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists.EBI
J Med Chem 45: 4737-47 (2002)
Salk Institute
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.EBI
J Med Chem 45: 4724-31 (2002)
Universita Di Camerino
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).EBI
J Med Chem 45: 4716-23 (2002)
University Of Pennsylvania
Imidazole inhibitors of cytokine release: probing substituents in the 2 position.EBI
J Med Chem 45: 4695-705 (2002)
Eberhard-Karls-University TüBingen
Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase.EBI
J Med Chem 45: 4669-78 (2002)
Bristol-Myers Squibb
Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.EBI
J Med Chem 45: 4655-68 (2002)
Universit£
Cyclosporins: structure-activity relationships for the inhibition of the human FPR1 formylpeptide receptor.EBI
J Med Chem 45: 4613-28 (2002)
Strasbourg 1 University
Cyclosporins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC transporter.EBI
J Med Chem 45: 4598-612 (2002)
Strasbourg 1 University
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.EBI
J Med Chem 45: 4594-7 (2002)
Friedrich-Alexander University
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.EBI
J Med Chem 45: 4589-93 (2002)
Merck
Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors.BDB
J Am Chem Soc 124: 11852-3 (2002)
Millennium Pharmaceuticals
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.EBI
Bioorg Med Chem Lett 12: 3009-13 (2002)
Merck Frosst Centre For Therapeutic Research
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.EBI
Bioorg Med Chem Lett 12: 3001-4 (2002)
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.EBI
Bioorg Med Chem Lett 12: 2997-3000 (2002)
Merck Research Laboratories
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.EBI
Bioorg Med Chem Lett 12: 2993-6 (2002)
University Of California
Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors.BDB
Bioorg Med Chem Lett 12: 2989-92 (2002)
Wyeth Research
Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.EBI
Bioorg Med Chem Lett 12: 2977-80 (2002)
Glaxosmithkline
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.EBI
Bioorg Med Chem Lett 12: 2973-5 (2002)
Idun Pharmaceuticals
Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.EBI
Bioorg Med Chem Lett 12: 2969-71 (2002)
Idun Pharmaceuticals
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines.EBI
Bioorg Med Chem Lett 12: 2963-7 (2002)
Wyeth Research
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.EBI
Bioorg Med Chem Lett 12: 2957-61 (2002)
Wyeth Research
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.EBI
Bioorg Med Chem Lett 12: 2935-9 (2002)
Cv Therapeutics
Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.EBI
Bioorg Med Chem Lett 12: 2931-4 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates.EBI
Bioorg Med Chem Lett 12: 2925-30 (2002)
Corvas International
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).EBI
Bioorg Med Chem Lett 12: 2919-23 (2002)
Abbott Laboratories
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.EBI
Bioorg Med Chem Lett 12: 2913-7 (2002)
Genentech
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.EBI
Bioorg Med Chem Lett 12: 2907-11 (2002)
Universit£
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.EBI
Bioorg Med Chem Lett 12: 2893-7 (2002)
Wyeth Research
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.EBI
Bioorg Med Chem Lett 12: 2887-91 (2002)
Celera
Albumin affinity tags increase peptide half-life in vivo.EBI
Bioorg Med Chem Lett 12: 2883-6 (2002)
Genentech
Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase.EBI
Bioorg Med Chem Lett 12: 2879-82 (2002)
Bristol-Myers Squibb Pri
Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.EBI
Bioorg Med Chem Lett 12: 2875-8 (2002)
Bayer Research Center
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine.EBI
Bioorg Med Chem Lett 12: 2871-3 (2002)
Kyorin Pharmaceutical
Benzodiazepine inhibitors of the MMPs and TACE.EBI
Bioorg Med Chem Lett 12: 2867-70 (2002)
Wyeth Research
Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.EBI
Bioorg Med Chem Lett 12: 2859-61 (2002)
Upres Ea 1085
Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.EBI
Bioorg Med Chem Lett 12: 2855-8 (2002)
Merck Research Laboratories
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.EBI
Bioorg Med Chem Lett 12: 2829-31 (2002)
Cephalon
Development of potent and selective dipeptidyl peptidase II inhibitors.EBI
Bioorg Med Chem Lett 12: 2825-8 (2002)
University Of Antwerp (Uia)
Convenient synthesis and evaluation of enzyme inhibitory activity of several N-alkyl-, N-phenylalkyl, and cyclic isourea derivatives of 5a-carba-alpha-DL-fucopyranosylamine.EBI
Bioorg Med Chem Lett 12: 2811-4 (2002)
Keio University
Structural basis for Chk1 inhibition by UCN-01.BDB
J Biol Chem 277: 46609-15 (2002)
Glaxosmithkline
Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).EBI
Pharm Res 19: 1244-7 (2002)
University Of California
Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors.EBI
J Med Chem 45: 4581-4 (2002)
University Of Kuopio
Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis.EBI
J Med Chem 45: 4571-80 (2002)
Takeda Chemical Industries
4-Substituted D-glutamic acid analogues: the first potent inhibitors of glutamate racemase (MurI) enzyme with antibacterial activity.EBI
J Med Chem 45: 4559-70 (2002)
Eli Lilly
Inactivation and inhibition of gamma-aminobutyric acid aminotransferase by conformationally restricted vigabatrin analogues.EBI
J Med Chem 45: 4531-9 (2002)
Northwestern University
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.EBI
J Med Chem 45: 4513-23 (2002)
Kyowa Hakko Kogyo
Enhancement of nucleoside cytotoxicity through nucleotide prodrugs.EBI
J Med Chem 45: 4505-12 (2002)
Southern Research Institute
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.EBI
J Med Chem 45: 4471-84 (2002)
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B.EBI
J Med Chem 45: 4443-59 (2002)
Novo Nordisk
Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.EBI
J Med Chem 45: 4419-32 (2002)
Research And Development
A sorbitol dehydrogenase inhibitor of exceptional in vivo potency with a long duration of action: 1-(R)-[4-[4-(4,6-dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl]ethanol.EBI
J Med Chem 45: 4398-401 (2002)
Pfizer
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.EBI
J Med Chem 45: 4395-7 (2002)
Abbott Laboratories
A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge.EBI
J Med Chem 45: 4391-4 (2002)
University Of Naples Federico Ii
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.EBI
J Med Chem 45: 4383-6 (2002)
Eli Lilly
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.EBI
J Med Chem 45: 4379-82 (2002)
Women'S Health Research Institute
High affinity antagonists of the vanilloid receptor.BDB
Mol Pharmacol 62: 947-56 (2002)
National Cancer Institute-Bethesda
Identification of a mechanism by which the methylmercury antidotes N-acetylcysteine and dimercaptopropanesulfonate enhance urinary metal excretion: transport by the renal organic anion transporter-1.EBI
Mol Pharmacol 62: 921-6 (2002)
University Of Rochester School Of Medicine
Interaction of cytochrome P450 3A inhibitors with P-glycoprotein.EBI
J Pharmacol Exp Ther 303: 323-32 (2002)
St. Jude Children'S Research Hospital
Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate.EBI
J Pharmacol Exp Ther 303: 308-13 (2002)
Avmax
Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.BDB
J Pharmacol Exp Ther 303: 29-35 (2002)
University Of Arkansas
[Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine].BDB
Encephale 28: 350-5 (2002)
Emory University
A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity.BDB
FASEB J 16: 1829-31 (2002)
Chul
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.EBI
Bioorg Med Chem Lett 12: 2781-4 (2002)
National Institutes Of Health
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.BDB
Bioorg Med Chem Lett 12: 2767-70 (2002)
Merck Research Laboratories
8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors.BDB
Bioorg Med Chem Lett 12: 2761-5 (2002)
Wyeth-Ayerst Research
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 12: 2753-6 (2002)
University Of Alberta
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.EBI
Bioorg Med Chem Lett 12: 2719-22 (2002)
Merck Sharp & Dohme Research Laboratories
Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains.EBI
Bioorg Med Chem Lett 12: 2711-4 (2002)
Mogam Biotechnology Research Institute
Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 2: substitution of the glycine part.EBI
Bioorg Med Chem Lett 12: 2703-5 (2002)
University Of Antwerp (Uia)
Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.EBI
Bioorg Med Chem Lett 12: 2695-8 (2002)
Ghent University
Analogue based design of MMP-13 (Collagenase-3) inhibitors.EBI
Bioorg Med Chem Lett 12: 2689-93 (2002)
Gvk Biosciences
Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zinc binding functions.BDB
Bioorg Med Chem Lett 12: 2667-72 (2002)
Universita Degli Studi Di Firenze
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter.EBI
J Med Chem 45: 4371-4 (2002)
Niddk
Inhibition of the antibacterial target UDP-(3-O-acyl)-N-acetylglucosamine deacetylase (LpxC): isoxazoline zinc amidase inhibitors bearing diverse metal binding groups.EBI
J Med Chem 45: 4359-70 (2002)
Duke University
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).EBI
J Med Chem 45: 4344-9 (2002)
Purdue University
2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.EBI
J Med Chem 45: 4310-20 (2002)
Novartis Research Institute Vienna
Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR).EBI
J Med Chem 45: 4276-81 (2002)
Universita' Degli Studi Di Siena
N-[(2-Sulfo)-9-fluorenylmethoxycarbonyl](3)-gentamicin C(1) is a long-acting prodrug derivative.EBI
J Med Chem 45: 4264-70 (2002)
Institute Of Science
Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase.EBI
J Med Chem 45: 4254-63 (2002)
Instituto De Qu£Mica M£Dica (Csic)
Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid.EBI
J Med Chem 45: 4240-5 (2002)
The Royal Danish School Of Pharmacy
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.EBI
J Med Chem 45: 4222-39 (2002)
Takeda Chemical Industries
Synthesis of a novel series of benzocycloalkene derivatives as melatonin receptor agonists.EBI
J Med Chem 45: 4212-21 (2002)
Takeda Chemical Industries
Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.EBI
J Med Chem 45: 4202-11 (2002)
University Of Gda£?Sk
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.EBI
J Med Chem 45: 4171-87 (2002)
Novo Nordisk Research And Development
DrugScore meets CoMFA: adaptation of fields for molecular comparison (AFMoC) or how to tailor knowledge-based pair-potentials to a particular protein.EBI
J Med Chem 45: 4153-70 (2002)
Philipps-Universit£T Marburg
Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors.EBI
J Med Chem 45: 4128-39 (2002)
Universidad De Navarra
Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter.EBI
J Med Chem 45: 4119-27 (2002)
National Institute On Drug Abuse-Intramural Research Program/Nih
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.EBI
J Med Chem 45: 4110-8 (2002)
Drew University
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.EBI
J Med Chem 45: 4097-109 (2002)
Drew University
Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.EBI
J Med Chem 45: 4094-6 (2002)
Johnson & Johnson Pharmaceutical Research & Development
Purine and pyrimidine (P2) receptors as drug targets.EBI
J Med Chem 45: 4057-93 (2002)
National Institute Of Diabetes
Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.BDB
Chembiochem 3: 897-901 (2002)
New York University
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.BDB
Eur J Pharmacol 450: 191-202 (2002)
Schering-Plough Research Institute
A quick diversity-oriented amide-forming reaction to optimize P-subsite residues of HIV protease inhibitors.BDB
Chem Biol 9: 891-6 (2002)
The Scripps Research Institute
X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.BDB
Biochemistry 41: 10810-8 (2002)
Weizmann Institute Of Science
New flavonol oligoglycosides and polyacylated sucroses with inhibitory effects on aldose reductase and platelet aggregation from the flowers of Prunus mume.EBI
J Nat Prod 65: 1151-5 (2002)
Kyoto Pharmaceutical University
Naturally occurring cembranes from an Australian sarcophyton species.EBI
J Nat Prod 65: 1147-50 (2002)
Astrazeneca R&D Griffith University
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.BDB
Proc Natl Acad Sci U S A 99: 11934-9 (2002)
Case Western Reserve University
Conformationally constrained nicotines: polycyclic, bridged, and spiro-annulated analogues as novel ligands for the nicotinic acetylcholine receptor.EBI
J Med Chem 45: 4047-54 (2002)
Vienna University Of Technology
Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.EBI
J Med Chem 45: 4038-46 (2002)
Columbia University
Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter.EBI
J Med Chem 45: 4029-37 (2002)
Research Triangle Institute
Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.EBI
J Med Chem 45: 4000-10 (2002)
Freie Universit£T Berlin
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.EBI
J Med Chem 45: 3972-83 (2002)
Astrazeneca Pharmaceuticals
Divalent and trivalent alpha-ketocarboxylic acids as inhibitors of protein tyrosine phosphatases.EBI
J Med Chem 45: 3946-52 (2002)
Brown University
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.EBI
J Med Chem 45: 3934-45 (2002)
Instituto De Qu£Mica M£Dica (Csic)
Synthesis and evaluation of Glypsi(PO(2)R-N)Pro-containing pseudopeptides as novel inhibitors of the human cyclophilin hCyp-18.EBI
J Med Chem 45: 3928-33 (2002)
Departement D'Ingenierie Et D'Etudes Des Proteines
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.BDB
J Med Chem 45: 3905-27 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Chiral N,N-disubstituted trifluoro-3-amino-2-propanols are potent inhibitors of cholesteryl ester transfer protein.EBI
J Med Chem 45: 3891-904 (2002)
Pharmacia
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).EBI
J Med Chem 45: 3878-90 (2002)
Gsk
Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography.EBI
J Med Chem 45: 3865-77 (2002)
Pfizer
Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.EBI
J Med Chem 45: 3854-64 (2002)
Schering-Plough Research Institute
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.EBI
J Med Chem 45: 3844-53 (2002)
University Of Bologna
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.EBI
J Med Chem 45: 3829-35 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.EBI
J Med Chem 45: 3820-3 (2002)
University Of Maryland
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.EBI
J Med Chem 45: 3813-5 (2002)
Biovitrum
Effects of pyridine ring substitutions on affinity, efficacy, and subtype selectivity of neuronal nicotinic receptor agonist epibatidine.BDB
J Pharmacol Exp Ther 302: 1246-52 (2002)
University Of Miami
The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors.EBI
Bioorg Med Chem Lett 12: 2643-6 (2002)
The Schering Plough Research Institute
Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.EBI
Bioorg Med Chem Lett 12: 2607-9 (2002)
Universidade De Vigo
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.EBI
Bioorg Med Chem Lett 12: 2603-6 (2002)
Glaxosmithkline
8-Aryl xanthines potent inhibitors of phosphodiesterase 5.EBI
Bioorg Med Chem Lett 12: 2587-90 (2002)
Novartis Horsham Research Centre
Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor.EBI
Bioorg Med Chem Lett 12: 2583-6 (2002)
Merck Frosst Centre For Therapeutic Research
Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade.EBI
Bioorg Med Chem Lett 12: 2569-72 (2002)
Organon Laboratories
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.EBI
Bioorg Med Chem Lett 12: 2565-8 (2002)
Organon Laboratories
Dihydroquinolines as novel n-NOS inhibitors.EBI
Bioorg Med Chem Lett 12: 2561-4 (2002)
Schering
Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group.EBI
Bioorg Med Chem Lett 12: 2553-6 (2002)
University Of Antwerp (Uia)
Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles: new selective ligands of the 5-HT(7) receptor.BDB
Bioorg Med Chem Lett 12: 2549-52 (2002)
Meiji Seika Kaisha
Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis.EBI
Bioorg Med Chem Lett 12: 2545-8 (2002)
Atherogenics
A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.EBI
Bioorg Med Chem Lett 12: 2535-9 (2002)
Universit£
Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.EBI
Bioorg Med Chem Lett 12: 2519-22 (2002)
F. Hoffmann-La Roche
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.EBI
Bioorg Med Chem Lett 12: 2515-8 (2002)
Merck Sharp And Dohme Research Laboratories
Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe.EBI
Bioorg Med Chem Lett 12: 2501-5 (2002)
University Of Nottingham
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.BDB
Eur J Pharmacol 450: 37-41 (2002)
Aventis Pharmaceuticals
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.EBI
Biochem Biophys Res Commun 296: 644-50 (2002)
Kyushu University
Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators.EBI
J Med Chem 45: 3809-12 (2002)
University Of Bonn
Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.EBI
J Med Chem 45: 3805-8 (2002)
Otsuka Pharmaceutical
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.EBI
J Med Chem 45: 3794-804 (2002)
Bristol-Myers Squibb
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI
J Med Chem 45: 3772-93 (2002)
Millennium Pharmaceuticals
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.EBI
J Med Chem 45: 3755-64 (2002)
Boehringer Ingelheim Pharma
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.EBI
J Med Chem 45: 3746-54 (2002)
University Of California
N-Acylvanillamides: development of an expeditious synthesis and discovery of new acyl templates for powerful activation of the vanilloid receptor.EBI
J Med Chem 45: 3739-45 (2002)
Istituto Per La Chimica Di Molecole Di Interesse Biologico
Oxygenated metabolites of anandamide and 2-arachidonoylglycerol: conformational analysis and interaction with cannabinoid receptors, membrane transporter, and fatty acid amide hydrolase.EBI
J Med Chem 45: 3709-20 (2002)
Utrecht University
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.EBI
J Med Chem 45: 3703-8 (2002)
Nutrition Research Institute
The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.EBI
J Med Chem 45: 3692-702 (2002)
The Institute Of Cancer Research
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.BDB
J Med Chem 45: 3684-91 (2002)
National Institutes Of Health
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.EBI
J Med Chem 45: 3660-8 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor.EBI
J Med Chem 45: 3649-59 (2002)
Kennesaw State University
Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors.EBI
J Med Chem 45: 3639-48 (2002)
Abbott Laboratories
Alpha(1)-adrenoceptor antagonists. 4. Pharmacophore-based design, synthesis, and biological evaluation of new imidazo-, benzimidazo-, and indoloarylpiperazine derivatives.EBI
J Med Chem 45: 3603-11 (2002)
Università
Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation.BDB
J Med Chem 45: 3588-602 (2002)
University Of Marburg
Nonaromatic sulfonamide group as an ideal anchor for potent human carbonic anhydrase inhibitors: role of hydrogen-bonding networks in ligand binding and drug design.EBI
J Med Chem 45: 3583-7 (2002)
Universit£
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.EBI
J Med Chem 45: 3579-82 (2002)
TBA
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.EBI
J Med Chem 45: 3569-72 (2002)
TBA
Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase.EBI
Bioorg Med Chem Lett 12: 2487-90 (2002)
National Institute Of Diabetes And Digestive And Kidney Diseases
N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.EBI
Bioorg Med Chem Lett 12: 2479-82 (2002)
Hoffmann-La Roche
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.EBI
Bioorg Med Chem Lett 12: 2475-8 (2002)
Roche Research Center
Investigation of the PDZ domain ligand binding site using chemically modified peptides.EBI
Bioorg Med Chem Lett 12: 2471-4 (2002)
University Of California
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.EBI
Bioorg Med Chem Lett 12: 2463-5 (2002)
Merck Research Laboratories
1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT(7) receptor ligands.EBI
Bioorg Med Chem Lett 12: 2451-4 (2002)
Nps Pharmaceuticals
An improved synthesis of the C-linked glucuronide of N-(4-hydroxyphenyl)retinamide.EBI
Bioorg Med Chem Lett 12: 2447-50 (2002)
The Ohio State University
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.EBI
Bioorg Med Chem Lett 12: 2443-6 (2002)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.EBI
Bioorg Med Chem Lett 12: 2423-6 (2002)
Merck Research Laboratories
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.EBI
Bioorg Med Chem Lett 12: 2419-22 (2002)
Merck Research Laboratories
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.EBI
Bioorg Med Chem Lett 12: 2407-10 (2002)
Roche Research Center
C-3 Amido-indole cannabinoid receptor modulators.EBI
Bioorg Med Chem Lett 12: 2399-402 (2002)
Bristol-Myers Squibb
Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.EBI
Bioorg Med Chem Lett 12: 2391-4 (2002)
Kingston University
Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes.EBI
Bioorg Med Chem Lett 12: 2387-90 (2002)
University Of New Orleans
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.EBI
Bioorg Med Chem Lett 12: 2377-80 (2002)
Friedrich-Alexander University
Novel inhibitors of plasminogen activator inhibitor-1: development of new templates from diketopiperazines.EBI
Bioorg Med Chem Lett 12: 2367-70 (2002)
Xenova
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.EBI
Bioorg Med Chem Lett 12: 2355-8 (2002)
Schering-Plough Research Institute
Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry.EBI
Bioorg Med Chem Lett 12: 2349-53 (2002)
Minase Research Institute
Synthesis of [(2S,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]-5-methylfuran-4-carboxylic acid derivatives: new leads as selective beta-galactosidase inhibitors.EBI
Bioorg Med Chem Lett 12: 2335-9 (2002)
Universidad De Sevilla
A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.EBI
Bioorg Med Chem Lett 12: 2313-6 (2002)
Korea Institute Of Science & Technology
Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.EBI
Bioorg Med Chem Lett 12: 2291-4 (2002)
Fukui Research Institute
3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists.EBI
Bioorg Med Chem Lett 12: 2287-90 (2002)
Chinese Academy Of Sciences
3D-QSAR studies on 4-hydroxyphenylpyruvate dioxygenase inhibitors by comparative molecular field analysis (CoMFA).EBI
Bioorg Med Chem Lett 12: 2271-5 (2002)
Zhejiang University
L-Cysteine based N-type calcium channel blockers: structure-activity relationships of the C-terminal lipophilic moiety, and oral analgesic efficacy in rat pain models.EBI
Bioorg Med Chem Lett 12: 2267-9 (2002)
Minase Research Institute
Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor.EBI
Bioorg Med Chem Lett 12: 2263-6 (2002)
Universita' Di Firenze
Sequencing, modeling, and selective inhibition of Trypanosoma brucei hexokinase.BDB
Chem Biol 9: 839-47 (2002)
Universite Paul Sabatier
Agonodepsides a and B: two new depsides from a filamentous fungus F7524.EBI
J Nat Prod 65: 1037-8 (2002)
Institute Of Molecular And Cell Biology
Bioactive abietane and seco-abietane diterpenoids from Salvia prionitis.EBI
J Nat Prod 65: 1016-20 (2002)
Chinese Academy Of Sciences
Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.BDB
J Med Chem 45: 3558-68 (2002)
Guilford Pharmaceuticals
Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.EBI
J Med Chem 45: 3549-57 (2002)
Guilford Pharmaceuticals
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.EBI
J Med Chem 45: 3524-30 (2002)
Research Triangle Institute
Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity.EBI
J Med Chem 45: 3509-23 (2002)
Astrazeneca
Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid.EBI
J Med Chem 45: 3482-90 (2002)
Pfizer
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.EBI
J Med Chem 45: 3451-7 (2002)
Genentech
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.EBI
J Med Chem 45: 3440-50 (2002)
University Of Bonn
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.EBI
J Med Chem 45: 3418-29 (2002)
Menarini Ricerche
Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.EBI
J Med Chem 45: 3406-17 (2002)
Saarland University
Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.EBI
J Med Chem 45: 3394-405 (2002)
Boehringer Ingelheim Pharmaceuticals
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.BDB
J Med Chem 45: 3381-93 (2002)
University Of Newcastle
(4R,5S)/(4S,5R)-4,5-Bis(4-hydroxyphenyl)-2-imidazolines: ligands for the estrogen receptor with a novel binding mode.EBI
J Med Chem 45: 3356-65 (2002)
Free University Of Berlin
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.EBI
J Med Chem 45: 3337-44 (2002)
Instituto De QuíMica MéDica (Csic)
Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa?EBI
Pharm Res 19: 773-9 (2002)
The University Of Kansas
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?EBI
Pharm Res 19: 765-72 (2002)
The University Of Kansas
SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties.BDB
J Pharmacol Exp Ther 302: 731-41 (2002)
Sanofi-Synthelabo Recherche
Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors.BDB
J Pharmacol Exp Ther 302: 687-95 (2002)
University Of Kentucky
Characterization of methotrexate transport and its drug interactions with human organic anion transporters.EBI
J Pharmacol Exp Ther 302: 666-71 (2002)
Kyorin University
Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4.EBI
J Pharmacol Exp Ther 302: 645-50 (2002)
Dr. Margarete Fischer-Bosch-Institute Of Clinical Pharmacology
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.EBI
Eur J Pharm Sci 16: 159-65 (2002)
Kyoto Pharmaceutical University
Binding modes of two novel dinucleotide inhibitors of HIV-1 integrase.EBI
Bioorg Med Chem Lett 12: 2233-6 (2002)
The University Of Iowa
Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines.EBI
Bioorg Med Chem Lett 12: 2225-8 (2002)
Southern Research Institute
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.EBI
Bioorg Med Chem Lett 12: 2205-8 (2002)
Merck Research Laboratories
Design and synthesis of novel inhibitors of gelatinase B.EBI
Bioorg Med Chem Lett 12: 2201-4 (2002)
University Of California
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.EBI
Bioorg Med Chem Lett 12: 2197-200 (2002)
Merck Research Laboratories
Phosphonate and phosphinate analogues of N-acylated gamma-glutamylglutamate. potent inhibitors of glutamate carboxypeptidase II.EBI
Bioorg Med Chem Lett 12: 2189-92 (2002)
Guilford Pharmaceuticals
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 12: 2185-7 (2002)
Neurocrine Biosciences
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 12: 2179-83 (2002)
Neurocrine Biosciences
Rational design of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2(p185(erbB)) tyrosine kinases.BDB
Bioorg Med Chem Lett 12: 2153-7 (2002)
Sugen
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.EBI
Bioorg Med Chem Lett 12: 2145-8 (2002)
Johnson & Johnson Pharmaceutical Research And Development
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.EBI
Bioorg Med Chem Lett 12: 2141-4 (2002)
Merck Research Laboratories
Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase.EBI
Bioorg Med Chem Lett 12: 2137-40 (2002)
Bristol-Myers Squibb Pharmaceutical Research Institute
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.EBI
Bioorg Med Chem Lett 12: 2133-6 (2002)
Neurogen
Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.EBI
Bioorg Med Chem Lett 12: 2125-8 (2002)
The Schering Plough Research Institute
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.EBI
Bioorg Med Chem Lett 12: 2121-3 (2002)
Abbott Laboratories
Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.EBI
Bioorg Med Chem Lett 12: 2113-6 (2002)
Abbott