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Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.EBI
Bioorg Med Chem Lett 9: 97-102 (1999)
Universit£t Erlangen-N£rnberg
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.EBI
Bioorg Med Chem Lett 9: 91-6 (1999)
Novartis Pharmaceuticals
The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents.EBI
Bioorg Med Chem Lett 9: 75-8 (1999)
Eli Lilly and Company
Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.EBI
Bioorg Med Chem Lett 9: 43-8 (1999)
Instituto de Química Médica (CSIC)
A study of novel antiallergic agents with eosinophilic infiltration inhibiting action.EBI
Bioorg Med Chem Lett 9: 19-24 (1999)
Tokushima Bunri University
Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors.EBI
Bioorg Med Chem Lett 9: 7-12 (1999)
Schering-Plough Research Institute
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.EBI
J Med Chem 42: 526-31 (1999)
Eli Lilly and Company
Metallopeptidase inhibitors of tetanus toxin: A combinatorial approach.EBI
J Med Chem 42: 515-25 (1999)
University of Paris
Structure-activity relationships: analogues of the dicaffeoylquinic and dicaffeoyltartaric acids as potent inhibitors of human immunodeficiency virus type 1 integrase and replication.EBI
J Med Chem 42: 497-509 (1999)
University of California
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.EBI
J Med Chem 42: 490-6 (1999)
Università di Bari
Three-dimensional quantitative structure-activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices analysis to elucidate selectivity differences of inhibitors binding to trypsin, thrombin, and factor Xa.EBI
J Med Chem 42: 458-77 (1999)
University of Marburg
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists.EBI
J Med Chem 42: 427-37 (1999)
Recordati S.p.A.
A new class of pseudopeptide antagonists of the kinin B1 receptor containing alkyl spacers.EBI
J Med Chem 42: 409-14 (1999)
Institute of Mutagenesis and Differentiation
Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.EBI
J Med Chem 42: 400-4 (1999)
Sapienza University of Rome
Identification and characterization of m1 selective muscarinic receptor antagonists1.EBI
J Med Chem 42: 356-63 (1999)
Warner-Lambert Company
Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and alpha1 receptor binding affinity.EBI
J Med Chem 42: 336-45 (1999)
Angelini Ricerche S.p.A.
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.EBI
J Med Chem 42: 333-5 (1999)
University of Pennsylvania
Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes.EBI
Bioorg Med Chem Lett 8: 3689-92 (1999)
Research Triangle Institute
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.EBI
Bioorg Med Chem Lett 8: 3683-8 (1999)
Corvas International Inc
Benzothiopyran-4-one based reversible inhibitors of the human cytomegalovirus (HCMV) protease.EBI
Bioorg Med Chem Lett 8: 3677-82 (1999)
SmithKline Beecham Pharmaceuticals Ltd
Differential activity of rosiglitazone enantiomers at PPAR gamma.EBI
Bioorg Med Chem Lett 8: 3657-8 (1999)
Glaxo Wellcome Research and Development
Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system.EBI
Bioorg Med Chem Lett 8: 3649-52 (1999)
University of Maryland
Design and synthesis of novel conformationally restricted HIV protease inhibitors.EBI
Bioorg Med Chem Lett 8: 3637-42 (1999)
Vertex Pharmaceuticals Inc
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.EBI
Bioorg Med Chem Lett 8: 3631-6 (1999)
Vertex Pharmaceuticals Inc
(2Z,4E)-5-(5,6-dichloro-2-indolyl)-2-methoxy-N-(1,2,2,6,6- pentamethylpiperidin-4-yl)-2,4-pentadienamide, a novel, potent and selective inhibitor of the osteoclast V-ATPase.EBI
Bioorg Med Chem Lett 8: 3621-6 (1999)
SmithKline Beecham Research Unit
Tricyclic ureas: a new class of HIV-1 protease inhibitors.EBI
Bioorg Med Chem Lett 8: 3615-20 (1999)
DuPont Pharmaceuticals Company
The solid phase synthesis of a series of tri-substituted hydantoin ligands for the somatostatin SST5 receptor.EBI
Bioorg Med Chem Lett 8: 3609-14 (1999)
Glaxo Wellcome Cambridge Chemistry Laboratory
Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.EBI
Bioorg Med Chem Lett 8: 3603-8 (1999)
NV Organon Scientific Development Group
The discovery of orally available thrombin inhibitors: studies towards the optimisation of CGH1668.EBI
Bioorg Med Chem Lett 8: 3583-8 (1999)
Novartis Horsham Research Center
Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists.EBI
Bioorg Med Chem Lett 8: 3577-82 (1999)
Pfizer Inc
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.EBI
Bioorg Med Chem Lett 8: 3571-6 (1999)
Universidad de Santiago de Compostela
Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors.EBI
Bioorg Med Chem Lett 8: 3567-70 (1999)
University of Vigo
Unsymmetric nonpeptidic HIV protease inhibitors containing anthranilamide as a P2' ligand.EBI
Bioorg Med Chem Lett 8: 3537-42 (1999)
AIDS Drug Screening and Development Laboratory, SA
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.EBI
Bioorg Med Chem Lett 8: 3531-6 (1999)
Abbott Laboratories
Inhibition stereochemistry of hydroxamate inhibitors for thermolysin.EBI
Bioorg Med Chem Lett 8: 3515-8 (1999)
Pohang University of Science and Technology
Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5' and 8.EBI
Bioorg Med Chem Lett 8: 3505-10 (1999)
University of Washington
Design and synthesis of new secretory phospholipase A2 inhibitor of a phospholipid analog.EBI
Bioorg Med Chem Lett 8: 3495-8 (1999)
Kwansei Gakuin University
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.EBI
Bioorg Med Chem Lett 8: 3469-74 (1999)
Schering-Plough Research Institute
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 359: 7-10 (1999)
Schering-Plough Research Institute
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 359: 1-6 (1999)
Eli Lilly and Company
Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor.BDB
Ann N Y Acad Sci 861: 140-5 (1998)
Albany Medical College
2,6-Difluorophenol as a bioisostere of a carboxylic acid: bioisosteric analogues of gamma-aminobutyric acid.EBI
J Med Chem 42: 329-32 (1999)
Northwestern University
N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.EBI
J Med Chem 42: 312-23 (1999)
Nippon Steel Corporation
Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.EBI
J Med Chem 42: 305-11 (1999)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.EBI
J Med Chem 42: 260-6 (1999)
University College London
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.EBI
J Med Chem 42: 249-59 (1999)
Lindsley F. Kimball Research Institute
Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).EBI
J Med Chem 42: 210-2 (1999)
Ligand Pharmaceuticals Inc
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.EBI
J Med Chem 42: 202-5 (1999)
SmithKline Beecham Pharmaceuticals Ltd
Pharmacological treatment of obesity: therapeutic strategies.EBI
J Med Chem 42: 181-201 (1999)
The R. W. Johnson Pharmaceutical Research Institute
Potent 3-spiropiperidine growth hormone secretagogues.EBI
Bioorg Med Chem Lett 8: 107-12 (1999)
Merck Research Laboratories
Primary active transport of peptidic endothelin antagonists by rat hepatic canalicular membrane.EBI
J Pharmacol Exp Ther 288: 575-81 (1999)
University of Tokyo
Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella.EBI
J Nat Prod 62: 173-5 (1999)
Harbor Branch Oceanographic Institution
Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein.EBI
Jpn J Cancer Res 89: 1220-8 (1999)
Kobe University
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.EBI
J Med Chem 42: 173-7 (1999)
Università di Milano
Carboxy-substituted cinnamides: a novel series of potent, orally active LTB4 receptor antagonists.EBI
J Med Chem 42: 164-72 (1999)
Novartis Pharmaceuticals Corporation
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.BDB
J Med Chem 42: 135-52 (1999)
DuPont Pharmaceuticals Company
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and the alpha2-adrenoceptor.EBI
J Med Chem 42: 118-34 (1999)
University of Kansas
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.EBI
J Med Chem 42: 87-94 (1999)
Procter and Gamble Pharmaceuticals
Synthesis and structure-activity relationships of a new model of arylpiperazines. 4. 1-[omega-(4-Arylpiperazin-1-yl)alkyl]-3-(diphenylmethylene) - 2, 5-pyrrolidinediones and -3-(9H-fluoren-9-ylidene)-2, 5-pyrrolidinediones: study of the steric requirements of the terminal amide fragment on 5-HT1A aEBI
J Med Chem 42: 36-49 (1999)
Universidad Complutense
Potent inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands.EBI
J Med Chem 42: 25-35 (1999)
National Cancer Institute-Bethesda
Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.BDB
Br J Pharmacol 125: 1413-20 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Cloning and characterization of the human galanin GALR2 receptor.BDB
Peptides 19: 1771-81 (1998)
Synaptic Pharmaceutical Corporation
Trypanocidal bisbenzylisoquinoline alkaloids are inhibitors of trypanothione reductase.BDB
J Enzym Inhib 13: 1-9 (1998)
ORSTOM
Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor.BDB
J Med Chem 41: 5457-65 (1998)
University of Auckland
Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.EBI
J Med Chem 41: 5445-56 (1999)
Institut für Biochemie
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).EBI
J Med Chem 41: 5402-9 (1999)
Centro de Investigación Grupo Ferrer
New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities.EBI
J Med Chem 41: 5393-401 (1999)
Universit£ degli Studi di Torino
The 16,17-double bond is needed for irreversible inhibition of human cytochrome p45017alpha by abiraterone (17-(3-pyridyl)androsta-5, 16-dien-3beta-ol) and related steroidal inhibitors.EBI
J Med Chem 41: 5375-81 (1999)
Institute of Cancer Research
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounds.EBI
J Med Chem 41: 5362-74 (1999)
Eli Lilly and Company
Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability.EBI
J Med Chem 41: 5353-61 (1999)
University of Connecticut
Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.EBI
Bioorg Med Chem Lett 8: 3423-8 (1999)
Centre de Recherche Pierre Fabre
Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.EBI
Bioorg Med Chem Lett 8: 3409-14 (1999)
Warner-Lambert Company
Conformationally constrained analogues of diacylglycerol (DAG). 15. The indispensable role of the sn-1 and sn-2 carbonyls in the binding of DAG-lactones to protein kinase C (PK-C).EBI
Bioorg Med Chem Lett 8: 3403-8 (1999)
National Institutes of Health
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.EBI
Bioorg Med Chem Lett 8: 3365-70 (1999)
Ligand Pharmaceuticals Inc
Acceptor substrate-based selective inhibition of galactosyltransferases.EBI
Bioorg Med Chem Lett 8: 3359-64 (1999)
Scripps Research Institute
Chemoenzymatic synthesis of iminocyclitol derivatives: a useful library strategy for the development of selective fucosyltransfer enzymes inhibitors.EBI
Bioorg Med Chem Lett 8: 3353-8 (1999)
Scripps Research Institute
Potent inhibitors of the MAP kinase p38.EBI
Bioorg Med Chem Lett 8: 3335-40 (1998)
R. W. Johnson Pharmaceutical Research Institute
Synthesis of benzocycloalkane derivatives as new conformationally restricted ligands for melatonin receptors.EBI
Bioorg Med Chem Lett 8: 3325-30 (1999)
Paris-Sud University
A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity.BDB
Bioorg Med Chem Lett 8: 3321-4 (1998)
Gilead Sciences Inc
Potent, non-thiol inhibitors of farnesyltransferase.EBI
Bioorg Med Chem Lett 8: 3311-6 (1999)
Merck Research Laboratories
Aryl C-glycosides: physiologically stable glycomimetics of sialyl Lewis X.EBI
Bioorg Med Chem Lett 8: 3307-10 (1999)
Sankyo Co., Ltd
Restricting the flexibility of crosslinked, interfacial peptide inhibitors of HIV-1 protease.EBI
Bioorg Med Chem Lett 8: 3281-6 (1999)
Purdue University
Novel phosphate mimetics for the design of non-peptidyl inhibitors of protein tyrosine phosphatases.EBI
Bioorg Med Chem Lett 8: 3275-80 (1999)
University of Toronto
Thio-sugars. IV: Design and synthesis of S-linked fucoside analogs as a new class of alpha-L-fucosidase inhibitors.EBI
Bioorg Med Chem Lett 8: 3265-8 (1999)
University of Connecticut
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.EBI
Bioorg Med Chem Lett 8: 3251-6 (1999)
Abbott Laboratories
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.EBI
Bioorg Med Chem Lett 8: 3229-34 (1999)
Novartis Horsham Research Center
Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives.EBI
Bioorg Med Chem Lett 8: 3223-8 (1999)
GlaxoWellcome Medicines Research Center
Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.EBI
Bioorg Med Chem Lett 8: 3203-6 (1999)
Pharmacopeia Inc
Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications.EBI
Bioorg Med Chem Lett 8: 3193-8 (1999)
BioChem Therapeutic Inc.
Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model.EBI
Bioorg Med Chem Lett 8: 3171-6 (1999)
SmithKline Beecham Pharmaceuticals Ltd
Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists.EBI
Bioorg Med Chem Lett 8: 3165-70 (1999)
SmithKline Beecham Pharmaceuticals Ltd
Syntheses and antitumor activity of cis-restricted combretastatins: 5-membered heterocyclic analogues.EBI
Bioorg Med Chem Lett 8: 3153-8 (1998)
Ajinomoto Co. Inc
N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.EBI
Bioorg Med Chem Lett 8: 3149-52 (1999)
Research Triangle Institute
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI
Bioorg Med Chem Lett 8: 3143-8 (1999)
DuPont Pharmaceuticals Company
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.EBI
Bioorg Med Chem Lett 8: 3127-32 (1999)
Neurogen Corporation
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.EBI
Bioorg Med Chem Lett 8: 3111-6 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.EBI
Bioorg Med Chem Lett 8: 3093-6 (1999)
Washington University
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.EBI
Bioorg Med Chem Lett 8: 3087-92 (1999)
Merck Research Laboratories
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.EBI
Bioorg Med Chem Lett 8: 3081-6 (1999)
Merck Research Laboratories
Orally active indole N-oxide PDE4 inhibitors.EBI
Bioorg Med Chem Lett 8: 3053-8 (1998)
Rh£ne-Poulenc Rorer Central Research
Design, synthesis and biological activity of a pyrrolo [2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid.EBI
Bioorg Med Chem Lett 8: 3019-24 (1999)
Universit£ di Ferrara
Preparation of biotinylated allosamidins with strong chitinase inhibitory activities.EBI
Bioorg Med Chem Lett 8: 2987-90 (1998)
University of Tokyo
Synthesis of benzanilide derivatives as dual acting agents with alpha 1-adrenoceptor antagonistic action and steroid 5-alpha reductase inhibitory activity.EBI
Bioorg Med Chem Lett 8: 2967-72 (1998)
Zeria Pharmaceutical Co., Ltd.
Conformationally constrained NO synthase inhibitors: rigid analogs of L-N-iminoethylornithine.EBI
Bioorg Med Chem Lett 8: 2961-6 (1999)
Université de Haute-Alsace
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.EBI
Bioorg Med Chem Lett 8: 2955-60 (1999)
Glaxo Wellcome Research and Development
PDE4 inhibitors: new xanthine analogues.EBI
Bioorg Med Chem Lett 8: 2925-30 (1998)
Chiroscience Ltd
4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase.EBI
Bioorg Med Chem Lett 8: 2907-12 (1999)
Pharmacia & Upjohn
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.EBI
Bioorg Med Chem Lett 8: 2897-902 (1999)
Novo Nordisk A/S
Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.EBI
Bioorg Med Chem Lett 8: 2891-6 (1999)
Novartis Pharma AG
Synthesis of benzo[c]quinolizin-3-ones: selective non-steroidal inhibitors of steroid 5 alpha-reductase 1.EBI
Bioorg Med Chem Lett 8: 2871-6 (1999)
Universit£ di Firenze
Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain.EBI
Bioorg Med Chem Lett 8: 2865-70 (1999)
Novartis Pharma Inc
Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.EBI
Bioorg Med Chem Lett 8: 2859-64 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Synthesis and antiproliferative activity of a cyclic analog of dolastatin 10.EBI
Bioorg Med Chem Lett 8: 2855-8 (1999)
Laboratoire des M£canismes Mol£culaires des Communications Cellulaires (CNRS UPR 9023)
2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.EBI
Bioorg Med Chem Lett 8: 2849-54 (1999)
Eli Lilly and Company
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.EBI
Bioorg Med Chem Lett 8: 2839-44 (1999)
DuPont Pharmaceuticals Company
Design and synthesis of a pyridone-based phosphotyrosine mimetic.EBI
Bioorg Med Chem Lett 8: 2813-6 (1999)
Cadus Pharmaceutical Corporation
Design and synthesis of dipeptidyl alpha',beta'-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain.EBI
Bioorg Med Chem Lett 8: 2809-12 (1999)
University of Michigan
Exploration of beta-turn scaffolding motifs as components of sialyl Le(X) mimetics and their relevance to P-selectin.EBI
Bioorg Med Chem Lett 8: 2803-8 (1999)
Universit£ de Montr£al
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.EBI
Bioorg Med Chem Lett 8: 2797-802 (1999)
Abbott Laboratories
Sialyl Lewis X-polysaccharide conjugates: targeting inflammatory lesions.EBI
Bioorg Med Chem Lett 8: 2783-6 (1999)
Drug Delivery System Institute, Ltd.
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 8: 2777-82 (1999)
Merck Frosst Centre for Therapeutic Research
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).EBI
Bioorg Med Chem Lett 8: 2757-62 (1999)
Idun Pharmaceuticals, Inc.
Conformationally restricted carbamate inhibitors of horse serum butyrylcholinesterase.EBI
Bioorg Med Chem Lett 8: 2747-50 (1999)
National Chung-Hsing University
2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors.EBI
Bioorg Med Chem Lett 8: 2737-42 (1998)
Rh£ne-Poulenc Rorer
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.EBI
Bioorg Med Chem Lett 8: 2731-6 (1999)
Ligand Pharmaceuticals
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.EBI
Bioorg Med Chem Lett 8: 2719-24 (1999)
Boehringer Ingelheim (Canada) Ltd
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.EBI
Bioorg Med Chem Lett 8: 2715-8 (1999)
Neurogen Corporation
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.EBI
Bioorg Med Chem Lett 8: 2705-10 (1999)
DuPont Pharmaceuticals Company
Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI
Bioorg Med Chem Lett 8: 2689-94 (1999)
Merck Research Laboratory
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.EBI
Bioorg Med Chem Lett 8: 2685-8 (1999)
University of Michigan
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.EBI
Bioorg Med Chem Lett 8: 2681-4 (1999)
University of Michigan
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.EBI
Bioorg Med Chem Lett 8: 2675-80 (1999)
Wyeth-Ayerst Research Laboratory
Thalidomide analogs and PDE4 inhibition.EBI
Bioorg Med Chem Lett 8: 2669-74 (1998)
Celgene Corporation
The synthesis and biological activity of a novel series of diazepine MMP inhibitors.EBI
Bioorg Med Chem Lett 8: 2657-62 (1999)
Wyeth-Ayerst Research
P2-proline-derived inhibitors of calpain I.EBI
Bioorg Med Chem Lett 8: 2647-52 (1999)
Cephalon Inc
Aryl sulfonamides as selective PDE4 inhibitors.EBI
Bioorg Med Chem Lett 8: 2635-40 (1999)
Chiroscience Ltd
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.EBI
Bioorg Med Chem Lett 8: 2629-34 (1998)
Chiroscience Ltd
Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2.EBI
Bioorg Med Chem Lett 8: 2623-8 (1999)
GlaxoWellcome Medicines Research Center
Synthesis and binding of stable bisubstrate ligands for phosphoglycerate kinase.EBI
Bioorg Med Chem Lett 8: 2603-8 (1998)
University of Sheffield
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.EBI
Bioorg Med Chem Lett 8: 2589-94 (1999)
Cambridge University Forvie Site
N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists.EBI
Bioorg Med Chem Lett 8: 2583-8 (1999)
Freie Universit£t Berlin
Synthesis of boronic acid analogs of L-arginine as alternate substrates or inhibitors of nitric oxide synthase.EBI
Bioorg Med Chem Lett 8: 2573-6 (1999)
Université de Rennes 1
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.EBI
Bioorg Med Chem Lett 8: 2563-8 (1999)
Biotech Research Institute
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.EBI
Bioorg Med Chem Lett 8: 2521-6 (1999)
Schering-Plough Research Institute
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI
Bioorg Med Chem Lett 8: 2501-6 (1999)
Corvas International Inc
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.EBI
Bioorg Med Chem Lett 8: 2495-500 (1999)
Merck & Co.
The development of novel and selective p56lck tyrosine kinase inhibitors.EBI
Bioorg Med Chem Lett 8: 2489-94 (1999)
R. W. Johnson Pharmaceutical Research Institute
H-phosphonate derivatives as novel peptide deformylase inhibitors.EBI
Bioorg Med Chem Lett 8: 2479-82 (1999)
Ohio State University
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.EBI
Bioorg Med Chem Lett 8: 2467-72 (1999)
Merck & Co.
Templates for design of inhibitors for serine proteases: application of the program DOCK to the discovery of novel inhibitors for thrombin.EBI
Bioorg Med Chem Lett 8: 2463-6 (1999)
Wayne State University
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.EBI
Bioorg Med Chem Lett 8: 2457-62 (1999)
Solvay Pharma
N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4.EBI
Bioorg Med Chem Lett 8: 2451-6 (1999)
Pfizer Inc
NMR and topochemical studies of peptidomimetic HIV-I protease inhibitors containing a cis-epoxide amide isostere.EBI
Bioorg Med Chem Lett 8: 2423-6 (1999)
Biotech Research Institute
Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers.EBI
Bioorg Med Chem Lett 8: 2415-8 (1999)
Warner-Lambert Company
Synthesis of sialyl Lewis X mimetics using the Ugi four-component reaction.EBI
Bioorg Med Chem Lett 8: 2333-8 (1999)
Scripps Research Institute
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.EBI
Bioorg Med Chem Lett 8: 2321-6 (1999)
Molecumetics Ltd.
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.EBI
Bioorg Med Chem Lett 8: 2315-20 (1999)
Pharmacopeia Inc
Rapid optimization of an ICE inhibitor synthesis using multiple reaction conditions in a parallel array.EBI
Bioorg Med Chem Lett 8: 2309-14 (1999)
Warner-Lambert Company
Exploring structure-activity relationships around the phosphomannose isomerase inhibitor AF14049 via combinatorial synthesis.EBI
Bioorg Med Chem Lett 8: 2303-8 (1999)
Affymax Research Institute
Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.EBI
Bioorg Med Chem Lett 8: 2297-302 (1999)
University of California
Combinatorial chemistry: from peptides and peptidomimetics to small organic and heterocyclic compounds.EBI
Bioorg Med Chem Lett 8: 2273-8 (1999)
Institute for Molecular Studies
4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor.EBI
Bioorg Med Chem Lett 8: 2263-8 (1999)
Schering-Plough Research Institute
L-tryptophan urea amides as NK1/NK2 dual antagonists.EBI
Bioorg Med Chem Lett 8: 2259-62 (1999)
Merck Research Laboratories
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.EBI
Bioorg Med Chem Lett 8: 2253-8 (1999)
Merck Research Laboratories
Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630.EBI
Bioorg Med Chem Lett 8: 2247-52 (1999)
Takarazuka Research Institute
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.EBI
Bioorg Med Chem Lett 8: 2241-6 (1999)
Takarazuka Research Institute
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.EBI
Bioorg Med Chem Lett 8: 2235-40 (1999)
Berlex Biosciences
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.EBI
Bioorg Med Chem Lett 8: 2223-6 (1999)
Clemson University
Isoxazolylthioamides as potential immunosuppressants a combinatorial chemistry approach.EBI
Bioorg Med Chem Lett 8: 2203-8 (1999)
Novartis Pharma AG
Conformationally restricted analogues of nicotine and anabasine.EBI
Bioorg Med Chem Lett 8: 2173-8 (1999)
SIBIA Neurosciences Inc
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.EBI
Bioorg Med Chem Lett 8: 2169-72 (1999)
Boehringer Ingelheim Pharmaceuticals Inc
Novel H3 receptor antagonists. Sulfonamide homologs of histamine.EBI
Bioorg Med Chem Lett 8: 2157-62 (1999)
Schering-Plough Research Institute
Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT).EBI
Bioorg Med Chem Lett 8: 2149-50 (1999)
National Cancer Institute-Bethesda
Probing the importance of spacial and conformational domains in captopril analogs for angiotensin converting enzyme activity.EBI
Bioorg Med Chem Lett 8: 2123-8 (1999)
Universit£ de Montr£al
Synthesis of novel substituted pyridines as inhibitors of endothelin converting enzyme-1 (ECE-1).EBI
Bioorg Med Chem Lett 8: 2117-22 (1999)
Warner-Lambert Company
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.EBI
Bioorg Med Chem Lett 8: 2111-6 (1999)
Merck Research Laboratories
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.EBI
Bioorg Med Chem Lett 8: 2087-92 (1999)
Abbott Laboratories
Design and synthesis of conformationally-constrained MMP inhibitors.EBI
Bioorg Med Chem Lett 8: 2077-80 (1999)
Procter and Gamble Pharmaceuticals
Kampanols: novel Ras farnesyl-protein transferase inhibitors from Stachybotrys kampalensis.EBI
Bioorg Med Chem Lett 8: 2071-6 (1999)
Merck Research Laboratories
Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.EBI
Bioorg Med Chem Lett 8: 2067-70 (1999)
Warner-Lambert Company
Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[[(4-chlorophenyl)sulfonyl]-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists.EBI
Bioorg Med Chem Lett 8: 2061-6 (1999)
Pfizer Inc
SAR of novel biarylmethylamine dopamine D4 receptor ligands.EBI
Bioorg Med Chem Lett 8: 2033-8 (1999)
Darmstadt
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.EBI
Bioorg Med Chem Lett 8: 2027-32 (1999)
Institute for Bioorganic Research
General construction pattern of histamine H3-receptor antagonists: change of a paradigm.EBI
Bioorg Med Chem Lett 8: 2011-6 (1999)
Freie Universität Berlin
Actinomycin D, C2 and VII, inhibitors of Grb2-SHC interaction produced by Streptomyces.EBI
Bioorg Med Chem Lett 8: 2001-2 (1999)
Korea Research Institute of Bioscience and Biotechnology
Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells.EBI
Bioorg Med Chem Lett 8: 1997-2000 (1998)
University of Tokyo
Identification and characterization of m4 selective muscarinic antagonists.EBI
Bioorg Med Chem Lett 8: 1991-6 (1999)
Parke-Davis Pharmaceutical Research
Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid.EBI
Bioorg Med Chem Lett 8: 1985-90 (1999)
Eli Lilly and Company
A practical synthesis of 3-substituted delta 3,5(6)-steroids as new potential 5 alpha-reductase inhibitor.EBI
Bioorg Med Chem Lett 8: 1949-52 (1998)
Chinese Academy of Science
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives.EBI
Bioorg Med Chem Lett 8: 1943-8 (1999)
Eli Lilly and Company
4-Alkylpiperidines related to SR-48968: potent antagonists of the neurokinin-2 (NK2) receptor.EBI
Bioorg Med Chem Lett 8: 1935-40 (1999)
Zeneca Pharmaceuticals
SAR studies of diaryltriazoles against bacterial two-component regulatory systems and their antibacterial activities.EBI
Bioorg Med Chem Lett 8: 1929-34 (1998)
R. W. Johnson Pharmaceutical Research Institute
Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: pharmacophore identification based on the screening hit closantel.EBI
Bioorg Med Chem Lett 8: 1923-8 (1998)
R. W. Johnson Pharmaceutical Research Institute
Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]-benzothiazolidine derivatives as a potential gastric H+/K(+)-ATPase inhibitor.EBI
Bioorg Med Chem Lett 8: 1909-12 (1999)
Ajou University
17 alpha-alkyl- or 17 alpha-substituted benzyl-17 beta-estradiols: a new family of estrone-sulfatase inhibitors.EBI
Bioorg Med Chem Lett 8: 1891-6 (1999)
Laval University
Inhibition of HIV integrase by novel nucleotides bearing tricyclic bases.EBI
Bioorg Med Chem Lett 8: 1887-90 (1999)
University of Iowa
Novel cytokine release inhibitors. Part I: Triterpenes.EBI
Bioorg Med Chem Lett 8: 1883-6 (1999)
Rhóne-Poulenc Rorer Central Research
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.EBI
Bioorg Med Chem Lett 8: 1877-82 (1999)
Berlex Biosciences
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.EBI
Bioorg Med Chem Lett 8: 1867-72 (1998)
Rh£ne-Poulenc Rorer Central Research
Synthesis and anti-HIV activities of symmetrical N1,N3-dibenzyl-2-hydroxy-propane derivatives.EBI
Bioorg Med Chem Lett 8: 1861-6 (1999)
Université de la Méditerranée
Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.EBI
Bioorg Med Chem Lett 8: 1851-6 (1999)
Merck Sharp and Dohme Research Laboratories
Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.EBI
Bioorg Med Chem Lett 8: 1845-50 (1999)
Merck Sharp and Dohme Research Laboratories
Modeling, synthesis and biological activity of novel antifungal agents (1).EBI
Bioorg Med Chem Lett 8: 1819-24 (1998)
Nippon Roche Research Center
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.EBI
Bioorg Med Chem Lett 8: 1813-8 (1999)
National Taiwan University
Development of new chromanol antagonists of leukotriene D4.EBI
Bioorg Med Chem Lett 8: 1791-6 (1998)
Pfizer Inc
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.EBI
Bioorg Med Chem Lett 8: 1781-6 (1998)
Pfizer Inc
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.EBI
Bioorg Med Chem Lett 8: 1771-6 (1999)
Merck KGaA
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.EBI
Bioorg Med Chem Lett 8: 1767-70 (1999)
Novo Nordisk A/S
Conformationally constrained analogues of diacylglycerol (DAG). 14. Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement.EBI
Bioorg Med Chem Lett 8: 1757-62 (1999)
National Cancer Institute-Bethesda
Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents.EBI
Bioorg Med Chem Lett 8: 1745-50 (1999)
DuPont Pharmaceuticals Company
Neuronorm is a potent and water soluble neurokinin A receptor antagonist.EBI
Bioorg Med Chem Lett 8: 1735-40 (1999)
Universit£ di Napoli Federico II
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.EBI
Bioorg Med Chem Lett 8: 1719-24 (1999)
Merck Research Laboratories
Peptide-based inhibitors of the hepatitis C virus serine protease.EBI
Bioorg Med Chem Lett 8: 1713-8 (1999)
Boehringer Ingelheim (Canada) Ltd
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.EBI
Bioorg Med Chem Lett 8: 1697-702 (1999)
Merck Research Laboratories
Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction.EBI
Bioorg Med Chem Lett 8: 1689-92 (1998)
GlaxoWellcome S.p.A.
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.EBI
Bioorg Med Chem Lett 8: 1683-6 (1999)
Biotech Research Institute
Identification of a potent analogue of Nazumamide A through iteration of combinatorial tetrapeptide libraries.EBI
Bioorg Med Chem Lett 8: 1669-72 (1999)
Central Drug Research Institute
Synthesis and acetylcholinesterase inhibitory activity of (+/-)-14-fluorohuperzine A.EBI
Bioorg Med Chem Lett 8: 1661-4 (1999)
Chinese Academy of Sciences
Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.EBI
Bioorg Med Chem Lett 8: 1649-54 (1999)
R. W. Johnson Pharmaceutical Research Institute
Adenosine deaminase inhibitors. Synthesis and biological evaluation of aralkyladenines (ARADS).EBI
Bioorg Med Chem Lett 8: 1639-42 (1999)
University of Rhode Island
A new series of cyclic amino acids as inhibitors of S-adenosyl L-methionine synthetase.EBI
Bioorg Med Chem Lett 8: 1629-34 (1999)
UMR 6519
Diarylsulfonamides as selective, non-peptidic thrombin inhibitors.EBI
Bioorg Med Chem Lett 8: 1613-8 (1999)
Pharmazeutisch-Chemisches Institut der Universität
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.EBI
Bioorg Med Chem Lett 8: 1595-600 (1999)
3-Dimensional Pharmaceuticals Inc
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist.EBI
Bioorg Med Chem Lett 8: 1569-74 (1999)
Università degli Studi
Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid.EBI
Bioorg Med Chem Lett 8: 1563-8 (1999)
Royal Danish School of Pharmacy
Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors.EBI
Bioorg Med Chem Lett 8: 1551-4 (1999)
Dainippon Pharmaceutical Co., Ltd
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.EBI
Bioorg Med Chem Lett 8: 1541-6 (1999)
Yamanouchi Pharmaceutical Co., Ltd
A potent dipeptide inhibitor of dipeptidyl peptidase IV.EBI
Bioorg Med Chem Lett 8: 1537-40 (1999)
Tanabe Seiyaku Co., Ltd
Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold.EBI
Bioorg Med Chem Lett 8: 1531-6 (1998)
Solvay Pharma
Evaluation of phosphorus-containing inhibitors of gamma-glutamyl hydrolase.EBI
Bioorg Med Chem Lett 8: 1521-4 (1999)
San Francisco State University
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.EBI
Bioorg Med Chem Lett 8: 1511-6 (1999)
Medivir AB
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.EBI
Bioorg Med Chem Lett 8: 1499-502 (1999)
Parke-Davis Pharmaceutical Research
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).EBI
Bioorg Med Chem Lett 8: 1477-82 (1999)
Institute for Drug Research
Inhibition of electric eel acetylcholinesterase by porphin compounds.EBI
Bioorg Med Chem Lett 8: 1467-70 (1999)
Taejon National University of Technology
5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series.EBI
Bioorg Med Chem Lett 8: 1461-6 (1999)
Institute
Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.EBI
Bioorg Med Chem Lett 8: 1449-54 (1999)
Fujisawa Pharmaceutical Co., Ltd
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.EBI
Bioorg Med Chem Lett 8: 1443-8 (1999)
Abbott Laboratories
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.EBI
Bioorg Med Chem Lett 8: 1437-42 (1999)
Boehringer Ingelheim (Canada) Ltd
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.EBI
Bioorg Med Chem Lett 8: 1419-24 (1999)
University of Paris
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.EBI
Bioorg Med Chem Lett 8: 1407-12 (1999)
Centre de Recherche Pierre Fabre
New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors.EBI
Bioorg Med Chem Lett 8: 1381-6 (1999)
Centre de Recherches de Croissy
Asymmetric synthesis of Boc-N-methyl-p-benzoyl-phenylalanine. Preparation of a photoreactive antagonist of substance P.EBI
Bioorg Med Chem Lett 8: 1369-74 (1999)
Universit£ P. et M. Curie
Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.EBI
Bioorg Med Chem Lett 8: 1353-8 (1999)
University of Bologna
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.EBI
Bioorg Med Chem Lett 8: 1343-8 (1999)
Merck Sharp Laboratory
Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors.EBI
Bioorg Med Chem Lett 8: 1337-42 (1999)
Centre de Recherche Pierre Fabre
A 3D-QSAR study on ginkgolides and their analogues with comparative molecular field analysis.EBI
Bioorg Med Chem Lett 8: 1291-6 (1999)
Chinese Academy of Sciences
A depsipeptide fungal metabolite inhibitor of cholesteryl ester transfer protein.EBI
Bioorg Med Chem Lett 8: 1277-80 (1999)
Schering-Plough Research Institute
Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.EBI
Bioorg Med Chem Lett 8: 1255-60 (1999)
Merck Frosst Centre for Therapeutic Research
1,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors.EBI
Bioorg Med Chem Lett 8: 1249-54 (1999)
Menarini Ricerche S.p.A.
Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones.EBI
Bioorg Med Chem Lett 8: 1237-42 (1999)
Pharmacia & Upjohn
Design and synthesis of bio-isosteres of thymidine triphosphate.EBI
Bioorg Med Chem Lett 8: 1211-4 (1999)
University of Wales Cardiff
Direct synthesis of [DOTA-DPhe1]-octreotide and [DOTA-DPhe1,Tyr3]-octreotide (SMT487): two conjugates for systemic delivery of radiotherapeutical nuclides to somatostatin receptor positive tumors in man.EBI
Bioorg Med Chem Lett 8: 1207-10 (1999)
Novartis Pharma AG
Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: novel inhibitors of COX-2.EBI
Bioorg Med Chem Lett 8: 1181-6 (1999)
Boehringer Ingelheim Pharmaceuticals Inc
Structure-activity relationships in 2-aminodiphenylsulfides against trypanothione reductase from Trypanosoma cruzi.EBI
Bioorg Med Chem Lett 8: 1175-80 (1999)
URA CNRS 1309
Synthesis and anti-inflammatory activity of chalcone derivatives.EBI
Bioorg Med Chem Lett 8: 1169-74 (1999)
Universidad de Valencia
The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.EBI
Bioorg Med Chem Lett 8: 1163-8 (1999)
Wyeth-Ayerst Research
Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors.EBI
Bioorg Med Chem Lett 8: 1157-62 (1999)
Affymax Research Institute
A novel super-potent neurokinin A receptor antagonist containing dehydroalanine.EBI
Bioorg Med Chem Lett 8: 1153-6 (1999)
Universit£ di Napoli Federico II
Substrate specificity of human prolyl-4-hydroxylase.EBI
Bioorg Med Chem Lett 8: 1139-44 (1999)
Cornell University
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.EBI
Bioorg Med Chem Lett 8: 1133-8 (1999)
Gliatech Inc
Serotonergic ergoline derivatives.EBI
Bioorg Med Chem Lett 8: 1117-22 (1999)
Pharmacia & Upjohn
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.EBI
Bioorg Med Chem Lett 8: 1107-12 (1999)
Merck Research Laboratories
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.EBI
Bioorg Med Chem Lett 8: 1101-6 (1999)
Merck Research Laboratories
The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.BDB
Bioorg Med Chem Lett 8: 1077-82 (1998)
DuPont Pharmaceuticals Company
Potent antimitotic and cell growth inhibitory properties of substituted chalcones.EBI
Bioorg Med Chem Lett 8: 1051-6 (1999)
University of Manchester Institute of Science and Technology
Design and synthesis of a new type of non steroidal human aromatase inhibitors.EBI
Bioorg Med Chem Lett 8: 1041-4 (1999)
Centre d'Etudes et de Recherche sur le Médicament de Normandie
Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.EBI
Bioorg Med Chem Lett 8: 1019-22 (1999)
Kyushu University
Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.EBI
Bioorg Med Chem Lett 8: 399-404 (1998)
Rh£ne-Poulenc Rorer Central Research
Synthesis and 5 alpha-reductase inhibitory activity of 8-substituted benzo[f]quinolinones derived from palladium mediated coupling reactions.EBI
Bioorg Med Chem Lett 8: 395-8 (1999)
Eli Lilly and Company
A new strong inhibitor of beta-mannosidase.EBI
Bioorg Med Chem Lett 8: 371-2 (1999)
S.E.S.N.A.B., Pole Sciences et Technologie, Universit� de La Rochelle. therisod@icmo.u-psud.fr
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.EBI
Bioorg Med Chem Lett 8: 365-70 (1999)
Glaxo Wellcome Research and Development
Synthesis of novel cyclic protease inhibitors using Grubbs olefin metathesis.EBI
Bioorg Med Chem Lett 8: 357-60 (1999)
University of Wisconsin-Madison
Naphthalenebis[alpha,alpha-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases.EBI
Bioorg Med Chem Lett 8: 345-50 (1999)
University of Toronto
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.EBI
Bioorg Med Chem Lett 8: 333-8 (1999)
ProScript, Inc.
Inhibition of thermolysin with nitrone-bearing substrate analogs: a new type of thermolysin inhibitors.EBI
Bioorg Med Chem Lett 8: 323-6 (1999)
Pohang University of Science and Technology
Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.EBI
Bioorg Med Chem Lett 8: 307-12 (1999)
DuPont Pharmaceuticals Company
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.EBI
Bioorg Med Chem Lett 8: 301-6 (1999)
DuPont Pharmaceuticals Company
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.EBI
Bioorg Med Chem Lett 8: 295-300 (1999)
Wyeth-Ayerst Research Laboratories
Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates.EBI
Bioorg Med Chem Lett 8: 289-94 (1999)
Warner-Lambert Company
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.EBI
Bioorg Med Chem Lett 8: 281-4 (1999)
Pfizer Inc
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.EBI
Bioorg Med Chem Lett 8: 261-6 (1999)
Novartis Pharma Inc
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.EBI
Bioorg Med Chem Lett 8: 249-54 (1999)
Abbott Laboratories
Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.EBI
Bioorg Med Chem Lett 8: 243-8 (1999)
Schering-Plough Research Institute
Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.EBI
Bioorg Med Chem Lett 8: 209-14 (1999)
CV Therapeutics Inc
Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.EBI
Bioorg Med Chem Lett 8: 195-8 (1999)
Purdue University
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.EBI
Bioorg Med Chem Lett 8: 175-8 (1998)
Rh£ne-Poulenc Rorer Central Research
S-aryl cysteine S,S-dioxides as inhibitors of mammalian kynureninase.EBI
Bioorg Med Chem Lett 8: 133-8 (1999)
Glaxo Wellcome Research and Development
Investigations of azapeptides as mimetics of Leu-enkephalin.EBI
Bioorg Med Chem Lett 8: 117-20 (1999)
Scripps Research Institute
DNA gyrase inhibitory activity of ellagic acid derivatives.EBI
Bioorg Med Chem Lett 8: 97-100 (1998)
R. W. Johnson Pharmaceutical Research Institute
Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) bearing a pyrazole ring.EBI
Bioorg Med Chem Lett 8: 81-6 (1999)
Fujisawa Pharmaceutical Co., Ltd
5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.EBI
Bioorg Med Chem Lett 8: 65-70 (1999)
Novartis Pharma AG
Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.EBI
Bioorg Med Chem Lett 8: 63-4 (1999)
Cinc
High affinity phenylglycinol-based NK1 receptor antagonists.EBI
Bioorg Med Chem Lett 8: 51-6 (1999)
Merck Sharp and Dohme Research Laboratories
Selective inhibition of low affinity IgE receptor (CD23) processing.EBI
Bioorg Med Chem Lett 8: 29-34 (1999)
SmithKline Beecham Pharmaceuticals Ltd
Hydroxamate-based inhibitors of low affinity IgE receptor (CD23) processing.EBI
Bioorg Med Chem Lett 8: 23-8 (1999)
SmithKline Beecham Pharmaceuticals Ltd
Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.EBI
Bioorg Med Chem Lett 8: 17-22 (1999)
Merck KGaA
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.EBI
Bioorg Med Chem Lett 8: 555-60 (1999)
University of Arizona
Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.EBI
Bioorg Med Chem Lett 8: 529-34 (1999)
Abbott Laboratories
Novel bisphosphonate inhibitors of phosphoglycerate kinase.EBI
Bioorg Med Chem Lett 8: 515-20 (1998)
Sheffield University
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds.EBI
Bioorg Med Chem Lett 8: 505-10 (1998)
Rhône-Poulenc Rorer
5-Aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 8: 493-8 (1999)
Novartis Pharma AG
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.EBI
Bioorg Med Chem Lett 8: 487-92 (1999)
Hong Kong University of Science and Technology
Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.EBI
Bioorg Med Chem Lett 8: 473-6 (1999)
Eli Lilly and Company
A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.EBI
Bioorg Med Chem Lett 8: 453-8 (1999)
Merck Frosst Center for Therapeutic Research
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.EBI
Bioorg Med Chem Lett 8: 447-52 (1999)
Georgetown University Medical Center
Structure activity relationship study of known inhibitors of the enzyme 5 alpha-reductase (5AR).EBI
Bioorg Med Chem Lett 8: 409-14 (1999)
Kingston University
Solid phase synthesis of a biased mini tetrapeptoid-library for the discovery of monodentate ITAM mimics as ZAP-70 inhibitors.EBI
Bioorg Med Chem Lett 8: 405-8 (1999)
Preclinical Research Novartis
Endothiopeptide inhibitors of HIV-1 protease.EBI
Bioorg Med Chem Lett 8: 699-704 (1999)
Purdue University
Diimidazo[1,2-c:4',5'-e]pyrimidines: N6-N1 conformationally restricted adenosines.EBI
Bioorg Med Chem Lett 8: 695-8 (1999)
Griffith University
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.EBI
Bioorg Med Chem Lett 8: 691-4 (1999)
Griffith University
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.BDB
Bioorg Med Chem Lett 8: 687-90 (1998)
University of Illinois at Chicago
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.EBI
Bioorg Med Chem Lett 8: 675-80 (1999)
Centre de Recherche Pierre Fabre
Syntheses of D- and L-myo-inositol 1,2,4,5-tetrakisphosphate and stereoselectivity of the I(1,4,5)P3 receptor binding.EBI
Bioorg Med Chem Lett 8: 659-62 (1999)
Pohang University of Science & Technology
Solid phase organic synthesis of polyamine derivatives and initial biological evaluation of their antitumoral activity.EBI
Bioorg Med Chem Lett 8: 635-40 (1998)
Universite de Rennes
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI
Bioorg Med Chem Lett 8: 631-4 (1999)
Biotech Research Institute
A novel series of N-(hexahydro-1,4-diazepin-6-yl) and N-(hexahydroazepin- 3-yl)benzamides with high affinity for 5-HT3 and dopamine D2 receptors.EBI
Bioorg Med Chem Lett 8: 619-24 (1999)
Dainippon Pharmaceutical Co., Ltd
An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase.EBI
Bioorg Med Chem Lett 8: 613-8 (1999)
Institute for Chemical Biology
1-[omega-(4-arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5- pyrrolidinediones as 5-HT1A receptor ligands: study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity.EBI
Bioorg Med Chem Lett 8: 581-6 (1999)
Universidad Complutense
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.EBI
Bioorg Med Chem Lett 8: 575-80 (1999)
Istituto di Strutturistica Chimica G. Giacomello
1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.EBI
Bioorg Med Chem Lett 8: 569-74 (1999)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro cancer cell growth inhibitory activity of monocyclic model compounds containing spongistatin triene side-chains.EBI
Bioorg Med Chem Lett 8: 567-8 (1999)
University of Pennsylvania
Synthesis and 5 alpha-reductase inhibitory activities of benzofuran derivatives with a carbamoyl group.EBI
Bioorg Med Chem Lett 8: 561-6 (1999)
Sankyo Co., Ltd
Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases.EBI
Bioorg Med Chem Lett 8: 837-42 (1999)
DuPont Pharmaceuticals Company
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.EBI
Bioorg Med Chem Lett 8: 823-8 (1999)
DuPont Pharmaceuticals Company
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.EBI
Bioorg Med Chem Lett 8: 817-22 (1999)
Merck Research Laboratories
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.EBI
Bioorg Med Chem Lett 8: 799-804 (1999)
National Institute of Diabetes
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases.BDB
Bioorg Med Chem Lett 8: 793-8 (1998)
Institut Curie
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.EBI
Bioorg Med Chem Lett 8: 775-80 (1999)
DuPont Pharmaceuticals Company
(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist.EBI
Bioorg Med Chem Lett 8: 765-70 (1999)
Eli Lilly and Company
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.EBI
Bioorg Med Chem Lett 8: 745-50 (1999)
Ligand Pharmaceuticals
Epoxide derivatives of pipecolic acid and proline are inhibitors of pipecolate oxidase.EBI
Bioorg Med Chem Lett 8: 739-44 (1999)
Oregon State University
Solid phase synthesis of benzylamine-derived sulfonamide library.EBI
Bioorg Med Chem Lett 8: 735-8 (1999)
Biotech Research Institute
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.EBI
Bioorg Med Chem Lett 8: 725-30 (1999)
Pfizer Inc
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups.EBI
Bioorg Med Chem Lett 8: 715-20 (1999)
DuPont Pharmaceuticals Company
Syntheses and kinetic evaluation of hydroxamate-based peptide inhibitors of glyoxalase I.EBI
Bioorg Med Chem Lett 8: 705-10 (1999)
University of Waterloo
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.EBI
Bioorg Med Chem Lett 8: 983-8 (1999)
R. W. Johnson Pharmaceutical Research Institute
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors.EBI
Bioorg Med Chem Lett 8: 979-82 (1999)
University of Illinois at Chicago
A 2-methyleneoxetane analog of orlistat demonstrating inhibition of porcine pancreatic lipase.EBI
Bioorg Med Chem Lett 8: 977-8 (1998)
University of Connecticut
Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.EBI
Bioorg Med Chem Lett 8: 965-70 (1999)
Novartis Pharma AG
Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).EBI
Bioorg Med Chem Lett 8: 959-64 (1999)
Ferring Research Institute Inc.
Peptide inhibitors of N-succinyl diaminopimelic acid aminotransferase (DAP-AT): a novel class of antimicrobial compounds.EBI
Bioorg Med Chem Lett 8: 945-50 (1999)
University of Bristol
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.EBI
Bioorg Med Chem Lett 8: 931-4 (1999)
Schering-Plough Research Institute
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.EBI
Bioorg Med Chem Lett 8: 925-30 (1999)
Georgetown University Medical Center
Peptidyl human heart chymase inhibitors. 2. Discovery of highly selective difluoromethylene ketone derivatives with Glu at P3 site.EBI
Bioorg Med Chem Lett 8: 919-24 (1999)
Green Cross Research Laboratories
Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.EBI
Bioorg Med Chem Lett 8: 913-8 (1999)
Green Cross Research Laboratories
Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase.EBI
Bioorg Med Chem Lett 8: 897-902 (1999)
Novartis Pharmaceuticals
Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.EBI
Bioorg Med Chem Lett 8: 891-6 (1999)
Abbott Laboratories
Structural analysis of inhibitor binding to human carbonic anhydrase II.BDB
Protein Sci 7: 2483-9 (1998)
University of Pennsylvania
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.BDB
J Pharmacol Exp Ther 287: 860-7 (1998)
Second Tokushima Institute of New Drug Research
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.EBI
J Med Chem 41: 5320-33 (1999)
Synaptic Pharmaceutical Corporation
Synthesis and potent antifolate activity and cytotoxicity of B-ring deaza analogues of the nonpolyglutamatable dihydrofolate reductase inhibitor Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl- L-ornithine (PT523).EBI
J Med Chem 41: 5310-9 (1999)
Harvard Medical School
Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.EBI
J Med Chem 41: 5272-86 (1999)
Western Maryland College
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain.EBI
J Med Chem 41: 5265-71 (1999)
Trinity College
Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).EBI
J Med Chem 41: 5247-56 (1999)
Newcastle University
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).EBI
J Med Chem 41: 5198-218 (1999)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.EBI
J Med Chem 41: 5188-97 (1999)
Research Triangle Institute
The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes.EBI
J Med Chem 41: 5177-87 (1999)
Kennesaw State University
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.EBI
J Med Chem 41: 5167-76 (1999)
Vrije Universiteit Brussel
Enantiospecific semisynthesis of (+)-almuheptolide-A, a novel natural heptolide inhibitor of the mammalian mitochondrial respiratory chain.EBI
J Med Chem 41: 5158-66 (1999)
Universidad de Valencia
Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists.EBI
J Med Chem 41: 5150-7 (1999)
Novo Nordisk A/S
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.EBI
J Med Chem 41: 5148-9 (1999)
Purdue University
Immunophilins: beyond immunosuppression.EBI
J Med Chem 41: 5119-43 (1999)
Guilford Pharmaceuticals Inc
Role of the cofactor calcium in the activation of outer membrane phospholipase A.BDB
Biochemistry 37: 16011-8 (1998)
Utrecht University
Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores.BDB
Naunyn Schmiedebergs Arch Pharmacol 358: 522-8 (1998)
King's College London
Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series.BDB
Bioorg Med Chem 6: 1835-50 (1998)
CNRS
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities.BDB
J Med Chem 41: 5113-7 (1998)
DuPont Pharmaceuticals Company
Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding.EBI
J Med Chem 41: 5084-93 (1999)
Virginia Commonwealth University
Design and synthesis of a series of 6-substituted-2-pyridinylmethylamine derivatives as novel, high-affinity, selective agonists at 5-HT1A receptors.EBI
J Med Chem 41: 5070-83 (1998)
Pierre Fabre Research Center
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.EBI
J Med Chem 41: 5055-69 (1998)
Glaxo Wellcome Research and Development
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.EBI
J Med Chem 41: 5037-54 (1998)
Glaxo Wellcome Research and Development
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.EBI
J Med Chem 41: 5020-36 (1999)
Glaxo Wellcome Research and Development
Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives.EBI
J Med Chem 41: 4995-5001 (1999)
Purdue University
Tetrahydro-isoquinoline-based factor Xa inhibitors.EBI
J Med Chem 41: 4983-94 (1999)
Boehringer Mannheim GmbH
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.EBI
J Med Chem 41: 4973-82 (1999)
Georgetown University Medical Center
Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization.EBI
J Med Chem 41: 4965-72 (1998)
Universit£t Regensburg
Characterization of novel N,N'-disubstituted piperazines as sigma receptor ligands.EBI
J Med Chem 41: 4950-7 (1999)
National Institute of Diabetes and Digestive and Kidney Diseases
N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies.EBI
J Med Chem 41: 4933-8 (1999)
Universit£ di Pisa
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.EBI
J Med Chem 41: 4911-4 (1999)
University of Minnesota
Muscarinic receptor binding sites of the M4 subtype in porcine lung parenchyma.BDB
Pharmacol Toxicol 83: 200-7 (1998)
Case Western Reserve University
Baicalein, an alpha-glucosidase inhibitor from Scutellaria baicalensis.EBI
J Nat Prod 61: 1413-5 (1999)
Hokkaido University
Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.EBI
J Nat Prod 61: 1410-2 (1999)
Virginia Polytechnic Institute and State University
Isolation and structure elucidation of new PKCalpha inhibitors from Pinus flexilis.EBI
J Nat Prod 61: 1407-9 (1998)
Virginia Polytechnic and State University
Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.EBI
J Nat Prod 61: 1356-60 (1999)
National University of Singapore
Inhibitory activity of unsaturated fatty acids and anacardic acids toward soluble tissue factor-factor VIIa complex.EBI
J Nat Prod 61: 1352-5 (1999)
Searle Discovery Research
Isolation of translactone-containing triterpenes with thrombin inhibitory activities from the leaves of Lantana camara.EBI
J Nat Prod 61: 1328-31 (1999)
Glaxo Wellcome Research and Development
Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.BDB
J Neurochem 71: 2558-64 (1998)
F. Hoffmann-La Roche Inc
Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.EBI
J Biol Chem 273: 32776-86 (1998)
Medical College of Georgia
Inhibition of human caspases by peptide-based and macromolecular inhibitors.BDB
J Biol Chem 273: 32608-13 (1998)
Merck Research Laboratories
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.EBI
J Med Chem 41: 4903-9 (1998)
Universitá di Bari
(+)-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-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.BDB
J Med Chem 41: 4890-902 (1998)
Schering-Plough Research Institute
Human telomerase inhibition by regioisomeric disubstituted amidoanthracene-9,10-diones.EBI
J Med Chem 41: 4873-84 (1998)
The Institute of Cancer Research
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.EBI
J Med Chem 41: 4854-60 (1998)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.EBI
J Med Chem 41: 4844-53 (1998)
University of Bologna
Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.EBI
J Med Chem 41: 4833-43 (1998)
Institut Jacques Monod (UMR CNRS 7592/Universités Paris VI and VII)
Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.EBI
J Med Chem 41: 4800-18 (1998)
Center in Molecular Toxicology and The Vanderbilt Cancer Center
Selective tight binding inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase via structure-based drug design.EBI
J Med Chem 41: 4790-9 (1998)
University of Washington
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.EBI
J Med Chem 41: 4767-76 (1998)
The University of Arizona
Synthesis of 7-benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine and novel derivatives free of positional isomers. Potent inhibitors of cAMP-specific phosphodiesterase and of malignant tumor cell growth.EBI
J Med Chem 41: 4733-43 (1998)
University of Kaiserslautern
Synthesis, activity, and molecular modeling of new 2, 4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors.EBI
J Med Chem 41: 4706-15 (1998)
EP811-CNRS
Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas.EBI
J Med Chem 41: 4693-705 (1998)
Northeast Louisiana University
Novel CDC25A phosphatase inhibitors from pyrolysis of 3-alpha-azido-B-homo-6-oxa-4-cholesten-7-one on silica gel.EBI
J Med Chem 41: 4677-80 (1998)
University of Arizona
Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors.BDB
Chem Biol 5: 597-608 (1998)
DuPont Pharmaceuticals Company
Transport of monoamine transmitters by the organic cation transporter type 2, OCT2.EBI
J Biol Chem 273: 30915-20 (1998)
University of Heidelberg
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.EBI
J Pharmacol Exp Ther 287: 800-5 (1998)
Kyoto University Hospital
Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides.BDB
J Pharmacol Exp Ther 287: 448-56 (1998)
DuPont Pharmaceuticals Company
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.EBI
J Med Chem 41: 4623-35 (1998)
Merck Sharp and Dohme Research Laboratories
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.EBI
J Med Chem 41: 4607-14 (1998)
Merck Research Laboratories
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation.EBI
J Med Chem 41: 4587-98 (1998)
Fujisawa Pharmaceutical Ltd.
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.EBI
J Med Chem 41: 4577-86 (1998)
Northwestern University Medical School
Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.EBI
J Med Chem 41: 4567-76 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Synthesis and enzymic evaluation of 4-mercapto-6-oxo-1, 4-azaphosphinane-2-carboxylic acid 4-oxide as an inhibitor of mammalian dihydroorotase.EBI
J Med Chem 41: 4550-5 (1998)
University of Sydney
Alkoxypsoralens, novel nonpeptide blockers of Shaker-type K+ channels: synthesis and photoreactivity.EBI
J Med Chem 41: 4542-9 (1998)
University of Kiel
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.EBI
J Med Chem 41: 4533-41 (1998)
Duquesne University
Three-dimensional quantitative structure-activity relationship study of the cannabimimetic (aminoalkyl)indoles using comparative molecular field analysis.EBI
J Med Chem 41: 4521-32 (1998)
Sanofi Research Division
Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.EBI
J Med Chem 41: 4492-501 (1998)
Merck Research Laboratories
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.EBI
J Med Chem 41: 4486-91 (1998)
University of Minnesota
Synthesis and antitumor activity of new glycosides of epipodophyllotoxin, analogues of etoposide, and NK 611.EBI
J Med Chem 41: 4475-85 (1998)
UMR 176 CNRS/Institut Curie
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.EBI
J Med Chem 41: 4466-74 (1998)
Merck Research Laboratories
Pharmacophoric search and 3D-QSAR comparative molecular field analysis studies on agonists of melatonin sheep receptors.EBI
J Med Chem 41: 4453-65 (1998)
Universit£ d'Orl£ans
Highly potent bisphosphonate ligands for phosphoglycerate kinase.EBI
J Med Chem 41: 4439-52 (1998)
University of Sheffield
TROTEC-1: a new high-affinity ligand for labeling of the dopamine transporter.EBI
J Med Chem 41: 4429-32 (1998)
Institut f£r Bioanorganische und Radiopharmazeutische Chemie
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB
Regul Pept 29-37 (1998)
Uppsala University
Cloning and functional expression of the guinea pig neuropeptide Y Y2 receptor.BDB
Regul Pept 23-8 (1998)
Uppsala University
The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein.EBI
Hepatology 28: 1341-6 (1998)
University of Toronto
A new series of S-adenosyl-L-methionine synthetase inhibitors.BDB
J Enzym Inhib 13: 361-7 (1998)
Laboratoire de chimie bioorganique
New alkaloids from the papua new guinean sponge agelas nakamurai EBI
J Nat Prod 61: 1310-2 (1998)
Kagoshima University
Activity-guided isolation of steroidal alkaloid antiestrogen-binding site inhibitors from Pachysandra procumbens.EBI
J Nat Prod 61: 1257-62 (1998)
University of Illinois at Chicago
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.EBI
J Nat Prod 61: 1212-5 (1998)
Uppsala University
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 3. Discovery of a novel series of N-alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas with weak toxicological effects on adrenal glands.EBI
J Med Chem 41: 4408-20 (1998)
Fujisawa Pharmaceutical Co., Ltd
Potent cyano and carboxamido side-chain analogues of 1', 1'-dimethyl-delta8-tetrahydrocannabinol.EBI
J Med Chem 41: 4400-7 (1998)
Organix Inc
CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors.EBI
J Med Chem 41: 4385-99 (1998)
University of Texas at Austin
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.BDB
J Med Chem 41: 4365-77 (1998)
Parke-Davis Pharmaceutical Research
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.EBI
J Med Chem 41: 4354-9 (1998)
Ligand Pharmaceuticals Inc
Design of peptidomimetics that inhibit the association of phosphatidylinositol 3-kinase with platelet-derived growth factor-beta receptor and possess cellular activity.EBI
J Med Chem 41: 4329-42 (1998)
Warner-Lambert Company
Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.EBI
J Med Chem 41: 4309-16 (1998)
Chugai Pharmaceutical Company, Ltd.
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.EBI
J Med Chem 41: 4301-8 (1998)
Takeda Chemical Industries, Ltd
Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase.EBI
J Med Chem 41: 4288-300 (1998)
Abbott Laboratories
Studies on selectin blockers. 7. Structure-activity relationships of sialyl Lewis X mimetics based on modified Ser-Glu dipeptides.EBI
J Med Chem 41: 4279-87 (1998)
Kanebo
Design of new topoisomerase II inhibitors based upon a quinobenzoxazine self-assembly model.EBI
J Med Chem 41: 4273-8 (1998)
The University of Texas at Austin
Quantitative structure-activity relationships of 2, 4-diamino-5-(2-X-benzyl)pyrimidines versus bacterial and avian dihydrofolate reductase.EBI
J Med Chem 41: 4261-72 (1998)
University of California
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.EBI
J Med Chem 41: 4251-60 (1998)
Wyeth-Ayerst Research
Design of benzamidine-type inhibitors of factor Xa.EBI
J Med Chem 41: 4240-50 (1998)
Institut für Biochemie
Axially chiral N-benzyl-N,7-dimethyl-5-phenyl-1, 7-naphthyridine-6-carboxamide derivatives as tachykinin NK1 receptor antagonists: determination of the absolute stereochemical requirements.EBI
J Med Chem 41: 4232-9 (1998)
Takeda Chemical Industries, Ltd
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.EBI
J Med Chem 41: 4216-23 (1998)
SW 8 Rh£ne-Poulenc Rorer Central Research
Derivation of a pharmacophore model for anandamide using constrained conformational searching and comparative molecular field analysis.EBI
J Med Chem 41: 4207-15 (1998)
Saint Louis University School of Medicine
Synthesis and evaluation of N-[11C]methylated analogues of epibatidine as tracers for positron emission tomographic studies of nicotinic acetylcholine receptors.EBI
J Med Chem 41: 4199-206 (1998)
National Institute on Drug Abuse
6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor.EBI
J Med Chem 41: 4196-8 (1998)
The R. W. Johnson Pharmaceutical Research Institute
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.EBI
J Med Chem 41: 4190-5 (1998)
Takeda Chemical Industries, Ltd
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.EBI
J Med Chem 41: 4186-9 (1998)
University of Bologna
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.EBI
J Med Chem 41: 4181-5 (1998)
Astra Arcus USA
SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.BDB
Br J Pharmacol 125: 202-8 (1998)
SmithKline Beecham Pharmaceuticals Ltd
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.EBI
J Med Chem 41: 4171-6 (1998)
Freie Universität Berlin
N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.EBI
J Med Chem 41: 4165-70 (1998)
University of Crete
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.EBI
J Med Chem 41: 4150-60 (1998)
University of Bologna
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.EBI
J Med Chem 41: 4143-9 (1998)
Research Triangle Institute
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.EBI
J Med Chem 41: 4130-42 (1998)
University of Wisconsin-Milwaukee
Novel, highly potent aldose reductase inhibitors: (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4- tetrahydropyrrolo[1,2-a]pyrazine -4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and its congeners.EBI
J Med Chem 41: 4118-29 (1998)
Dainippon Pharmaceutical Company, Ltd.
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a] pyridine moiety.EBI
J Med Chem 41: 4062-79 (1998)
Fujisawa Pharmaceutical Company, Ltd
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man.EBI
J Med Chem 41: 4053-61 (1998)
Fujisawa Pharmaceutical Company, Ltd
New platelet fibrinogen receptor glycoprotein IIb-IIIa antagonists: orally active series of N-alkylated amidines with a 6,6-bicyclic template.EBI
J Med Chem 41: 4036-52 (1998)
Mitsui Pharmaceuticals Inc.
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.EBI
J Med Chem 41: 4021-35 (1998)
Rhône-Poulenc Rorer
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.EBI
J Med Chem 41: 4001-11 (1998)
University of Vienna
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.EBI
J Med Chem 41: 3994-4000 (1998)
Vrije Universiteit
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.EBI
J Med Chem 41: 3987-93 (1998)
Vrije Universiteit
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.BDB
J Med Chem 41: 3976-86 (1998)
University of Bologna
Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins.EBI
J Med Chem 41: 3972-5 (1998)
F. Hoffmann-La Roche Inc
Structure-based design of beta-lactamase inhibitors. 1. Synthesis and evaluation of bridged monobactams.EBI
J Med Chem 41: 3961-71 (1998)
F. Hoffmann-La Roche Inc
Geometrically and conformationally restrained cinnamoyl compounds as inhibitors of HIV-1 integrase: synthesis, biological evaluation, and molecular modeling.EBI
J Med Chem 41: 3948-60 (1998)
Sapienza University of Rome
N-[omega-(Tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine are highly potent and selective sigma1 or sigma2 ligands.EBI
J Med Chem 41: 3940-7 (1998)
Università di Bari
Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.EBI
J Med Chem 41: 3928-39 (1998)
Yale University
Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.EBI
J Med Chem 41: 3923-7 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.EBI
J Med Chem 41: 3919-22 (1998)
GlaxoWellcome Medicines Research Centre
Reduced folate derivatives are endogenous substrates for cMOAT in rats.EBI
Am J Physiol 275: 789-96 (1998)
University of Tokyo
Electrophysiological characteristics of the proton-coupled peptide transporter PEPT2 cloned from rat brain.EBI
Am J Physiol 275: 967-75 (1998)
Medical College of Georgia
Structural basis of inhibitor selectivity in MAP kinases.BDB
Structure 6: 1117-28 (1998)
University of Texas at Dallas
Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir.EBI
Biochem Biophys Res Commun 250: 246-51 (1998)
State University of New Jersey
Thermodynamic analysis of the binding of the polyglutamate chain of 5-formyltetrahydropteroylpolyglutamates to serine hydroxymethyltransferase.BDB
Biochemistry 37: 13536-42 (1998)
Virginia Commonwealth University
Effect of modulators on the ATPase activity and vanadate nucleotide trapping of human P-glycoprotein.EBI
Biochem Pharmacol 56: 719-27 (1998)
Eli Lilly and Company
Novel peptidyl phosphorus derivatives as inhibitors of human calpain I.EBI
J Med Chem 41: 3912-6 (1998)
Cephalon Inc
Naamidine A is an antagonist of the epidermal growth factor receptor and an in vivo active antitumor agent.EBI
J Med Chem 41: 3909-11 (1998)
University of Utah
Selective inhibitors of human lactate dehydrogenases and lactate dehydrogenase from the malarial parasite Plasmodium falciparum.EBI
J Med Chem 41: 3879-87 (1998)
University of New Mexico School of Medicine
Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosine analogues (4'-haloacetylene analogues derived from adenosine).EBI
J Med Chem 41: 3857-64 (1998)
Brigham Young University
Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study.EBI
J Med Chem 41: 3831-44 (1998)
Universit£ degli Studi di Milano
Inhibition of monoamine oxidase-B by condensed pyridazines and pyrimidines: effects of lipophilicity and structure-activity relationships.EBI
J Med Chem 41: 3812-20 (1998)
Université de Neuchâtel
Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV.EBI
J Med Chem 41: 3793-803 (1998)
Pharmacia & Upjohn
Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors. Use of L-mannaric acid as a peptidomimetic scaffold.EBI
J Med Chem 41: 3782-92 (1998)
Linköping University
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.EBI
J Med Chem 41: 3763-72 (1998)
Universita' di Siena
Proton-coupled oligopeptide transport by rat renal cortical brush border membrane vesicles: a functional analysis using ACE inhibitors to determine the isoform of the transporter.EBI
Biochim Biophys Acta 1373: 277-81 (1998)
University of Oxford
Synthesis and characterization of heteroarotinoids demonstrate structure specificity relationships.EBI
J Med Chem 41: 3753-7 (1998)
University of Oklahoma Health Sciences Center
Bicyclic acylguanidine Na+/H+ antiporter inhibitors.EBI
J Med Chem 41: 3736-47 (1998)
Merck KGaA
Novel orally active growth hormone secretagogues.EBI
J Med Chem 41: 3705-14 (1998)
Novo Nordisk A/S
2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling.EBI
J Med Chem 41: 3690-8 (1998)
National Institute on Drug Abuse
2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.EBI
J Med Chem 41: 3675-83 (1998)
Pfizer Inc
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.EBI
J Med Chem 41: 3664-74 (1998)
Novartis Pharma AG
Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives.EBI
J Med Chem 41: 3645-54 (1998)
Sanofi Winthrop Inc.
2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.BDB
J Med Chem 41: 3624-34 (1998)
Universita degli Studi di Milano
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.EBI
J Med Chem 41: 3609-23 (1998)
Washington University
Classical/nonclassical hybrid cannabinoids: southern aliphatic chain-functionalized C-6beta methyl, ethyl, and propyl analogues.EBI
J Med Chem 41: 3596-608 (1998)
University of Hawaii
ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.EBI
J Med Chem 41: 3582-95 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Discovery of potent, achiral matrix metalloproteinase inhibitors.EBI
J Med Chem 41: 3568-71 (1998)
Procter and Gamble Pharmaceuticals
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.EBI
J Med Chem 41: 3563-7 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.EBI
J Med Chem 41: 3557-62 (1998)
Berlex Biosciences
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.EBI
J Med Chem 41: 3551-6 (1998)
Berlex Biosciences
Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.BDB
Proc Natl Acad Sci U S A 95: 10836-41 (1998)
Merck Research Laboratories
Cloned human and rat galanin GALR3 receptors. Pharmacology and activation of G-protein inwardly rectifying K+ channels.BDB
J Biol Chem 273: 23321-6 (1998)
Synaptic Pharmaceutical Corporation
Recent natural products based drug development: a pharmaceutical industry perspective.EBI
J Nat Prod 61: 1053-71 (1998)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis.EBI
J Nat Prod 61: 1046-8 (1998)
The University of Tokyo
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.BDB
Br J Pharmacol 124: 1300-6 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Pyrazole bioisosteres of leflunomide as B-cell immunosuppressants for xenotransplantation and chronic rejection: scope and limitations.EBI
J Med Chem 41: 3530-8 (1998)
Novartis Pharma AG
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.EBI
J Med Chem 41: 3515-29 (1998)
Procter & Gamble Pharmaceuticals
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.EBI
J Med Chem 41: 3507-14 (1998)
Hokkaido University
Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.EBI
J Med Chem 41: 3499-506 (1998)
University of Oregon
3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.EBI
J Med Chem 41: 3493-8 (1998)
University of Bristol
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.BDB
J Med Chem 41: 3467-76 (1998)
Upjohn
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.EBI
J Med Chem 41: 3461-6 (1998)
Ligand Pharmaceuticals Inc
Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.EBI
J Med Chem 41: 3442-9 (1998)
Novartis Pharma Inc
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.EBI
J Med Chem 41: 3426-34 (1998)
Duquesne University
Small molecular probes for G-protein-coupled C5a receptors: conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a.EBI
J Med Chem 41: 3417-25 (1998)
University of Queensland
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.EBI
J Med Chem 41: 3387-401 (1998)
Ciba-Geigy AG
4-Benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.EBI
J Med Chem 41: 3367-72 (1998)
Eisai Company, Ltd
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth.EBI
J Med Chem 41: 3303-6 (1998)
Georgetown University Medical Center
5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.EBI
Pharm Res 15: 1154-9 (1998)
University of Michigan
Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.EBI
J Med Chem 41: 3298-302 (1998)
Cambridge NeuroScience Inc
Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter.EBI
J Med Chem 41: 3293-7 (1998)
Organix Inc
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.BDB
J Med Chem 41: 3276-92 (1998)
Parke-Davis Pharmaceutical Research
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).EBI
J Med Chem 41: 3261-75 (1998)
Abbott Laboratories
1,4- and 2,6-disubstituted amidoanthracene-9,10-dione derivatives as inhibitors of human telomerase.EBI
J Med Chem 41: 3253-60 (1998)
The Institute of Cancer Research
Synthesis and comparison of the antiinflammatory activity of manoalide and cacospongionolide B analogues.EBI
J Med Chem 41: 3232-8 (1998)
Universit£ di Salerno
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.EBI
J Med Chem 41: 3220-31 (1998)
National University of Singapore
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.EBI
J Med Chem 41: 3210-9 (1998)
Merck Research Laboratories
Salicylhydrazine-containing inhibitors of HIV-1 integrase: implication for a selective chelation in the integrase active site.EBI
J Med Chem 41: 3202-9 (1998)
National Cancer Institute-Bethesda
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.EBI
J Med Chem 41: 3186-201 (1998)
National Institute of Diabetes
Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.EBI
J Med Chem 41: 3174-85 (1998)
Universit£ di Ferrara
2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.EBI
J Med Chem 41: 3159-73 (1998)
Novartis Institute for Medical Sciences
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.EBI
J Med Chem 41: 3128-41 (1998)
National Taiwan University
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.EBI
J Med Chem 41: 3103-27 (1998)
Merck Research Laboratories
Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with mu-opioid receptor in rat brain and CHO-mu/1 cell line.BDB
Peptides 19: 1091-8 (1998)
Hungarian Academy of Sciences
Molecular pharmacology of homologues of ibotenic acid at cloned metabotropic glutamic acid receptors.BDB
Eur J Pharmacol 350: 311-6 (1998)
The Royal Danish School of Pharmacy
Pharmacology of [3H]prostaglandin E1/[3H]prostaglandin E2 and [3H]prostaglandin F2alpha binding to EP3 and FP prostaglandin receptor binding sites in bovine corpus luteum: characterization and correlation with functional data.BDB
J Pharmacol Exp Ther 286: 1094-102 (1998)
Alcon Laboratories Inc
Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain.BDB
J Pharmacol Exp Ther 286: 1007-13 (1998)
Memorial Sloan-Kettering Cancer Center
Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist.BDB
J Pharmacol Exp Ther 286: 650-6 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine.EBI
Mol Pharmacol 54: 342-52 (1998)
Institut f£r Physiologie
Rat alpha3/beta4 subtype of neuronal nicotinic acetylcholine receptor stably expressed in a transfected cell line: pharmacology of ligand binding and function.BDB
Mol Pharmacol 54: 322-33 (1998)
Georgetown University
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.BDB
NIDA Res Monogr 178: 440-66 (1998)
SRI International
Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its"hydrolytic activity": synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine.EBI
J Med Chem 41: 3078-83 (1998)
Brigham Young University
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels.EBI
J Med Chem 41: 3048-61 (1998)
Cambridge NeuroScience Inc
Bis-substituted malonic acid hydroxamate derivatives as inhibitors of human neutrophil collagenase (MMP8).EBI
J Med Chem 41: 3041-7 (1998)
Boehringer Mannheim GmbH
A new approach to the design of novel inhibitors of Na+,K+-ATPase: 17alpha-substituted seco-D 5beta-androstane as cassaine analogues.EBI
J Med Chem 41: 3033-40 (1998)
Prassis Istituto di Ricerche Sigma-Tau
Novel combretastatin analogues effective against murine solid tumors: design and structure-activity relationships.EBI
J Med Chem 41: 3022-32 (1998)
Ajinomoto Company Ltd.
Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut.EBI
J Med Chem 41: 3015-21 (1998)
Pharmaceutical Research Center
Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-ArylthiomethyldipyridodiazepinonesBDB
J Med Chem 41: 2972-84 (1998)
Boehringer Ingelheim Pharmaceuticals Inc
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.BDB
J Med Chem 41: 2960-71 (1998)
Boehringer Ingelheim Pharmaceuticals Inc
Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria.EBI
J Med Chem 41: 2939-45 (1998)
The R. W. Johnson Pharmaceutical Research Institute
Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase.EBI
J Med Chem 41: 2934-8 (1998)
Pfizer Inc
Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.EBI
J Med Chem 41: 2928-31 (1998)
Pfizer Inc
Thermodynamics of binding of calcium, magnesium, and zinc to the N-methyl-D-aspartate receptor ion channel peptidic inhibitors, conantokin-G and conantokin-T.BDB
J Biol Chem 273: 19573-8 (1998)
University of Notre Dame
A new cacospongionolide inhibitor of human secretory phospholipase A2 from the Tyrrhenian sponge Fasciospongia cavernosa and absolute configuration of cacospongionolides.EBI
J Nat Prod 61: 931-5 (1998)
Istituto per la Chimica di Molecole di Interesse Biologico CNR
The inhibition of the reverse transcriptase of HIV-1 by the natural sulfoglycolipids from cyanobacteria: contribution of different moieties to their high potency.EBI
J Nat Prod 61: 891-5 (1998)
Tel-Aviv University
Phospholipase Cgamma1 inhibitory principles from the sarcotestas of Ginkgo biloba.EBI
J Nat Prod 61: 867-71 (1998)
Seoul National University
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI
Science 281: 533-538 (1998)
University of California
Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters.BDB
Eur J Pharmacol 349: 129-32 (1998)
McGill University
Prodrugs of nitroxyl and nitrosobenzene as cascade latentiated inhibitors of aldehyde dehydrogenase.EBI
J Med Chem 41: 2903-9 (1998)
St. Cloud State University
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.EBI
J Med Chem 41: 2882-91 (1998)
Boehringer Ingelheim (Canada) Ltd
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.EBI
J Med Chem 41: 2872-81 (1998)
Southern Research Institute
N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.EBI
J Med Chem 41: 2858-71 (1998)
Glaxo Wellcome Research and Development
Styrylquinoline derivatives: a new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells.EBI
J Med Chem 41: 2846-57 (1998)
Paris-Sud University
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.EBI
J Med Chem 41: 2835-45 (1998)
National Institute of Diabetes
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 1. Michael acceptor structure-activity studies.EBI
J Med Chem 41: 2806-18 (1998)
Agouron Pharmaceuticals Inc
Tripeptide aldehyde inhibitors of human rhinovirus 3C protease: design, synthesis, biological evaluation, and cocrystal structure solution of P1 glutamine isosteric replacements.EBI
J Med Chem 41: 2786-805 (1998)
Agouron Pharmaceuticals Inc
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.EBI
J Med Chem 41: 2779-85 (1998)
Ligand Pharmaceuticals Inc
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.EBI
J Med Chem 41: 2765-78 (1998)
Yamanouchi Pharmaceutical Company, Ltd
Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.EBI
J Med Chem 41: 2745-53 (1998)
Rhône-Poulenc Rorer
Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.EBI
J Med Chem 41: 2732-44 (1998)
Rh£ne-Poulenc Rorer
Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists.EBI
J Med Chem 41: 2709-19 (1998)
Eli Lilly and Company
Design, synthesis, and biological activities of potent and selective somatostatin analogues incorporating novel peptoid residues.EBI
J Med Chem 41: 2679-85 (1998)
University of California San Diego
Nucleosides and nucleotides. 177. 9-(6,7-dideoxy-beta-D-allo-hept-5- ynofuranosyl)adenine: a selective and potent ligand for P3 purinoceptor-like protein.EBI
J Med Chem 41: 2676-8 (1998)
Hokkaido University
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.EBI
J Med Chem 41: 2667-70 (1998)
Merck Sharp and Dohme Research Laboratories
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.EBI
J Med Chem 41: 2663-6 (1998)
Cephalon Inc
In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.BDB
J Pharmacol Exp Ther 286: 569-77 (1998)
Parke-Davis Pharmaceutical Research
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).EBI
J Pharmacol Exp Ther 286: 354-61 (1998)
University of California
Characterization of alpha1-adrenoceptor subtypes in the pig.BDB
Eur J Pharmacol 347: 301-9 (1998)
Uppsala University
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.BDB
Chem Biol 5: 299-306 (1998)
University of California San Francisco
[125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.BDB
Eur J Pharmacol 348: 311-20 (1998)
Novartis Pharma
N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.EBI
J Med Chem 41: 2651-6 (1998)
Merck Research Laboratories
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.EBI
J Med Chem 41: 2643-50 (1998)
New York University Medical Center
Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase.EBI
J Med Chem 41: 2636-42 (1998)
Abbott Laboratories
Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.EBI
J Med Chem 41: 2631-5 (1998)
University of California San Diego
In vitro platelet-activating factor receptor binding inhibitory activity of pinusolide derivatives: a structure-activity study.EBI
J Med Chem 41: 2626-30 (1998)
Seoul National University
Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.EBI
J Med Chem 41: 2588-603 (1998)
SUGEN, Inc.
Carbocyclic analogues of the potent cytidine deaminase inhibitor 1-(beta-D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine).EBI
J Med Chem 41: 2572-8 (1998)
National Cancer Institute-Bethesda
Homonojirimycin isomers and N-alkylated homonojirimycins: structural and conformational basis of inhibition of glycosidases.EBI
J Med Chem 41: 2565-71 (1998)
Hokuriku University
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptorsEBI
J Med Chem 41: 2537-52 (1998)
University of Wisconsin-Milwaukee
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.EBI
J Med Chem 41: 2524-36 (1998)
Warner-Lambert Company
Pharmacophores incorporating numerous excluded volumes defined by X-ray crystallographic structure in three-dimensional database searching: application to the thyroid hormone receptor.BDB
J Med Chem 41: 2503-12 (1998)
Karo Bio AB
Design of a new class of orally active fibrinogen receptor antagonists.EBI
J Med Chem 41: 2492-502 (1998)
Rhône-Poulenc Rorer
Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones.EBI
J Med Chem 41: 2461-80 (1998)
Hoechst Marion Roussel Inc
Structure-activity relationship studies of novel carbocyclic influenza neuraminidase inhibitors.BDB
J Med Chem 41: 2451-60 (1998)
Gilead Sciences Inc
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.EBI
J Med Chem 41: 2445-50 (1998)
The George Washington University Medical Center
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.EBI
J Med Chem 41: 2442-4 (1998)
Wyeth-Ayerst Research
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 357: 483-9 (1998)
Novartis Pharma AG
Doxorubicin- and daunorubicin-glutathione conjugates, but not unconjugated drugs, competitively inhibit leukotriene C4 transport mediated by MRP/GS-X pump.EBI
Biochem Biophys Res Commun 247: 859-63 (1998)
University of Texas M. D. Anderson Cancer Center
Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells.BDB
Br J Pharmacol 124: 485-92 (1998)
Universit&aagrove; degli Studi di Milano
Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica.EBI
J Nat Prod 61: 854-6 (1998)
The University of Tokyo
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.EBI
J Nat Prod 61: 709-12 (1998)
Universidad de Valencia
Calorimetric investigation of ethidium and netropsin binding to chicken erythrocyte chromatin.BDB
Biochemistry 37: 9119-26 (1998)
Universite de Liege
Synthesis and dopamine transporter affinity of the four stereoisomers of (+/-)-2-(methoxycarbonyl)-7-methyl-3-phenyl-7-azabicyclo[2.2.1]heptane.EBI
J Med Chem 41: 2430-5 (1998)
University of New Orleans
Optimizing the binding of fullerene inhibitors of the HIV-1 protease through predicted increases in hydrophobic desolvation.EBI
J Med Chem 41: 2424-9 (1998)
University of California
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.EBI
J Med Chem 41: 2411-23 (1998)
DuPont Pharmaceuticals Company
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas.EBI
J Med Chem 41: 2390-410 (1998)
Fujisawa Pharmaceutical Co., Ltd
2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies.EBI
J Med Chem 41: 2380-9 (1998)
University of Oklahoma Health Sciences Center
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.BDB
J Med Chem 41: 2371-9 (1998)
University of North Carolina at Chapel Hill
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.EBI
J Med Chem 41: 2361-70 (1998)
Wake Forest University School of Medicine
GPIIb/IIIa integrin antagonists with the new conformational restriction unit, trisubstituted beta-amino acid derivatives, and a substituted benzamidine structure.EBI
J Med Chem 41: 2345-60 (1998)
Nippon Steel Corporation
Auxiliary agents for the peroral administration of peptide and protein drugs: synthesis and evaluation of novel pepstatin analogues.EBI
J Med Chem 41: 2339-44 (1998)
Institute of Pharmaceutical Chemistry
Studies on selectin blockers. 6. Discovery of homologous fucose sugar unit necessary for E-selectin binding.EBI
J Med Chem 41: 2302-7 (1998)
Kanebo
Synthesis and glutathione S-transferase structure-affinity relationships of nonpeptide and peptidase-stable glutathione analogues.EBI
J Med Chem 41: 2278-88 (1998)
Université Sidi Mohamed Ben Abdellah
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.EBI
J Med Chem 41: 2268-77 (1998)
Pfizer Inc.
Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraints in peptide design.EBI
J Med Chem 41: 2252-60 (1998)
University of Arizona
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.EBI
J Med Chem 41: 2243-51 (1998)
Virginia Commonwealth University
A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors.EBI
J Med Chem 41: 2201-6 (1998)
National Institute of Diabetes and Digestive and Kidney Diseases
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.EBI
J Med Chem 41: 2194-200 (1998)
Affymax Research Institute
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.EBI
J Med Chem 41: 2180-3 (1998)
Pharmacia & Upjohn
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.EBI
J Med Chem 41: 2175-9 (1998)
Merck Research Laboratories
Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site.BDB
Bioorg Med Chem 6: 595-604 (1998)
Sankyo Co., Ltd
Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs.BDB
Am J Med 104: 413-21 (1998)
Dallas Department of Veterans Affairs Medical Center
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.EBI
J Med Chem 41: 2146-63 (1998)
Merck Research Laboratories
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity.EBI
J Med Chem 41: 2134-45 (1998)
Purdue University
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.EBI
J Med Chem 41: 2126-33 (1998)
Università di Ferrara
Selective inhibitors of monoamine oxidase (MAO). 5. 1-Substituted phenoxathiin inhibitors containing no nitrogen that inhibit MAO A by binding it to a hydrophobic site.EBI
J Med Chem 41: 2118-25 (1998)
The Wellcome Research Laboratories
Specific and irreversible cyclopeptide inhibitors of dipeptidyl peptidase IV activity of the T-cell activation antigen CD26.EBI
J Med Chem 41: 2100-10 (1998)
Universit£ de Versailles
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.BDB
J Med Chem 41: 2076-89 (1998)
Purdue University
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.EBI
J Med Chem 41: 2068-75 (1998)
3-Dimensional Pharmaceuticals Inc
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.EBI
J Med Chem 41: 2047-55 (1998)
National Institute of Diabetes and Digestive and Kidney Diseases
Newly synthesized L-enantiomers of 3'-fluoro-modified beta-2'-deoxyribonucleoside 5'-triphosphates inhibit hepatitis B DNA polymerases but not the five cellular DNA polymerases alpha, beta, gamma, delta, and epsilon nor HIV-1 reverse transcriptase.EBI
J Med Chem 41: 2040-6 (1998)
Max-Delbr�ck-Centrum f�r Molekulare Medizin
Arylpiperazines with serotonin-3 antagonist activity: a comparative molecular field analysis.EBI
J Med Chem 41: 2029-39 (1998)
Purdue University
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.EBI
J Med Chem 41: 2019-28 (1998)
DuPont Pharmaceuticals Company
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.EBI
J Med Chem 41: 2010-8 (1998)
Institut de Chimie Pharmaceutique Albert Lespagnol
Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors.EBI
J Med Chem 41: 1997-2009 (1998)
R. W. Johnson Pharmaceutical Research Institute
Melatonin receptor pharmacology: toward subtype specificity.BDB
Biol Cell 89: 531-7 (1997)
King's College London
GR196429: a nonindolic agonist at high-affinity melatonin receptors.BDB
J Pharmacol Exp Ther 285: 1239-45 (1998)
Glaxo Wellcome Research and Development, Ltd.
Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.EBI
Biochem Biophys Res Commun 246: 470-5 (1998)
Medical College of Georgia
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.BDB
Biochem Pharmacol 55: 1035-43 (1998)
Roche Bioscience
Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.BDB
J Neurochem 70: 2252-61 (1998)
Paris-Sud University
Energetic roles of hydrogen bonds at the ureido oxygen binding pocket in the streptavidin-biotin complex.BDB
Biochemistry 37: 7657-63 (1998)
University of Washington
Calorimetric studies of E. coli SSB protein-single-stranded DNA interactions. Effects of monovalent salts on binding enthalpy.BDB
J Mol Biol 278: 999-1014 (1998)
Washington University
The elucidation of somatostatin receptor functions: a current view.BDB
Rev Physiol Biochem Pharmacol 133: 55-108 (1998)
German Institute of Human Nutrition
Spongiacidins A-D, new bromopyrrole alkaloids from hymeniacidon sponge EBI
J Nat Prod 61: 693-5 (1998)
Hokkaido University
Isolation of 1-carboxymethylnicotinic acid from the marine sponge anthosigmella cf. raromicrosclera As a cysteine protease inhibitor1 EBI
J Nat Prod 61: 671-2 (1998)
The University of Tokyo
Cyclotheonamides E2 and E3, new potent serine protease inhibitors from the marine sponge of the genus Theonella.EBI
J Nat Prod 61: 667-70 (1998)
The University of Tokyo
Nitrogen-containing furanose and pyranose analogues from Hyacinthus orientalis.EBI
J Nat Prod 61: 625-8 (1998)
Hokuriku University
Petrosaspongiolides M-R: new potent and selective phospholipase A2 inhibitors from the New Caledonian marine sponge Petrosaspongia nigra.EBI
J Nat Prod 61: 571-5 (1998)
Universit£ degli Studi di Napoli"Federico II"
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.EBI
J Med Chem 41: 1980-90 (1998)
Research Triangle Institute
(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.EBI
J Med Chem 41: 1970-9 (1998)
University of Virginia
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.EBI
J Med Chem 41: 1962-9 (1998)
Georgetown University Medical Center
Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.EBI
J Med Chem 41: 1956-61 (1998)
University of North Carolina at Chapel Hill
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives.BDB
J Med Chem 41: 1943-55 (1998)
Eli Lilly and Company
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.EBI
J Med Chem 41: 1934-42 (1998)
Astra Arcus AB
Synthesis and structure-activity relationships of bafilomycin A1 derivatives as inhibitors of vacuolar H+-ATPase.EBI
J Med Chem 41: 1883-93 (1998)
SmithKline Beecham S.p.A.
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.EBI
J Med Chem 41: 1846-54 (1998)
Università degli Studi di Bari
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency.EBI
J Med Chem 41: 1764-76 (1998)
Abbott Laboratories
Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors.EBI
J Med Chem 41: 1752-63 (1998)
Warner-Lambert Company
Macrocyclic amino carboxylates as selective MMP-8 inhibitors.EBI
J Med Chem 41: 1749-51 (1998)
DuPont Pharmaceuticals Company
Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.EBI
J Med Chem 41: 1745-8 (1998)
DuPont Pharmaceuticals Company
Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.EBI
J Med Chem 41: 1741-4 (1998)
Novartis Pharma Inc
Agonist-induced up-regulation of alpha4beta2 nicotinic acetylcholine receptors in M10 cells: pharmacological and spatial definition.BDB
Mol Pharmacol 53: 950-62 (1998)
University of Bath
Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.BDB
Mol Psychiatry 3: 123-34 (1998)
University of Toronto
Novel thieno[2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase.EBI
J Med Chem 41: 1729-40 (1998)
University of Leipzig
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.EBI
J Med Chem 41: 1708-15 (1998)
Universit£ di Camerino
Isosteric analogues of nicotinamide adenine dinucleotide derived from furanfurin, thiophenfurin, and selenophenfurin as mammalian inosine monophosphate dehydrogenase (type I and II) inhibitors.EBI
J Med Chem 41: 1702-7 (1998)
Universit£ di Camerino
Inhibition of human alcohol dehydrogenases by formamides.EBI
J Med Chem 41: 1696-701 (1998)
The University of Iowa
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.EBI
J Med Chem 41: 1688-95 (1998)
Arizona State University
Conformationally defined retinoic acid analogues. 4. Potential new agents for acute promyelocytic and juvenile myelomonocytic leukemias.EBI
J Med Chem 41: 1679-87 (1998)
University of Alabama at Birmingham
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.EBI
J Med Chem 41: 1641-50 (1998)
Georgetown University Medical Center
Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.EBI
J Med Chem 41: 1631-40 (1998)
Universit£ Blaise Pascal
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.EBI
J Med Chem 41: 1613-8 (1998)
University of Grenoble
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.EBI
J Med Chem 41: 1598-612 (1998)
SmithKline Beecham Pharmaceuticals
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors.EBI
J Med Chem 41: 1581-97 (1998)
National Cancer Institute-Frederick
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.EBI
J Med Chem 41: 1574-80 (1998)
University of Catania
5-(5,6-Dichloro-2-indolyl)-2-methoxy-2,4-pentadienamides: novel and selective inhibitors of the vacuolar H+-ATPase of osteoclasts with bone antiresorptive activity.EBI
J Med Chem 41: 1568-73 (1998)
SmithKline Beecham S.p.A.
Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.EBI
J Med Chem 41: 1561-7 (1998)
Schering-Plough Research Institute
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.EBI
J Med Chem 41: 1557-60 (1998)
University of Camerino
In vitro binding properties in rat brain of [3H]Ro 25-6981, a potent and selective antagonist of NMDA receptors containing NR2B subunits.BDB
J Neurochem 70: 2147-55 (1998)
F. Hoffmann-La Roche Inc
Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15.EBI
J Med Chem 41: 1524-30 (1998)
UPR 9023 CNRS
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.EBI
J Med Chem 41: 1513-23 (1998)
Novartis Pharmaceuticals Corporation
Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation.EBI
J Med Chem 41: 1476-96 (1998)
University of Tokyo
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.EBI
J Med Chem 41: 1456-66 (1998)
National Institute of Diabetes
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.BDB
J Med Chem 41: 1446-55 (1998)
DuPont Pharmaceuticals Company
Development of a three-dimensional CysLT1 (LTD4) antagonist model with an incorporated amino acid residue from the receptor.EBI
J Med Chem 41: 1439-45 (1998)
Vrije Universiteit
Synthesis and structure-activity relationships of carboxyflavones as structurally rigid CysLT1 (LTD4) receptor antagonists.EBI
J Med Chem 41: 1428-38 (1998)
Vrije Universiteit
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.EBI
J Med Chem 41: 1409-16 (1998)
Duquesne University
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.EBI
J Med Chem 41: 1382-91 (1998)
University of Pennsylvania
Rational drug design approach for overcoming drug resistance: application to pyrimethamine resistance in malaria.EBI
J Med Chem 41: 1367-70 (1998)
University of Manchester
2-Iminohomopiperidinium salts as selective inhibitors of inducible nitric oxide synthase (iNOS).EBI
J Med Chem 41: 1361-6 (1998)
Pfizer Inc
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.EBI
J Med Chem 41: 1357-60 (1998)
Pharmacia & Upjohn
Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.BDB
Eur J Pharmacol 343: 67-77 (1998)
Hospital Saint-Antoine
Isolation of 1-Methylherbipoline Salts of Halisulfate-1 and of Suvanine as Serine Protease Inhibitors from a Marine Sponge, Coscinoderma mathewsiEBI
J Nat Prod 61: 248-50 (1998)
Aoyama Gakuin University
Selective Pneumocystis carinii dihydrofolate reductase inhibitors: design, synthesis, and biological evaluation of new 2,4-diamino-5-substituted-furo[2,3-d]pyrimidines.EBI
J Med Chem 41: 1263-71 (1998)
Duquesne University
Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole.EBI
J Med Chem 41: 1252-62 (1998)
University of Michigan
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.EBI
J Med Chem 41: 1218-35 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.EBI
J Med Chem 41: 1209-17 (1998)
Kanebo Ltd.
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.EBI
J Med Chem 41: 1205-8 (1998)
Merck & Co.
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.BDB
Chem Biol 5: 185-96 (1998)
Merck Research Laboratories
DNA polymerase and topoisomerase II inhibitors from Psoralea corylifolia.EBI
J Nat Prod 61: 362-6 (1998)
Ohio State University
5-Lipoxygenase and cyclooxygenase-1 inhibitory active compounds from Atractylodes lancea.EBI
J Nat Prod 61: 347-50 (1998)
Heinrich-Heine-Universität Düsseldorf
Pharmacophoric requirements for cannabinoid side chains: multiple bond and C1'-substituted delta 8-tetrahydrocannabinols.EBI
J Med Chem 41: 1195-200 (1998)
National Hellenic Research Foundation
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.EBI
J Med Chem 41: 1172-84 (1998)
Pfizer Inc
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents.EBI
J Med Chem 41: 1155-62 (1998)
University of North Carolina at Chapel Hill
Potent antagonists of somatostatin: synthesis and biology.EBI
J Med Chem 41: 1146-54 (1998)
Tulane University School of Medicine
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.EBI
J Med Chem 41: 1138-45 (1998)
University of Louvain
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.EBI
J Med Chem 41: 1124-37 (1998)
Procter & Gamble Pharmaceuticals
New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.EBI
J Med Chem 41: 1112-23 (1998)
Procter & Gamble Pharmaceuticals
Novel synthetic inhibitors of selectin-mediated cell adhesion: synthesis of 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-alpha-D- mannopyranosyloxy)phenyl]hexane (TBC1269).EBI
J Med Chem 41: 1099-111 (1998)
Texas Biotechnology Corporation
2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.EBI
J Med Chem 41: 1060-7 (1998)
Warner-Lambert Company
Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.EBI
J Med Chem 41: 1042-9 (1998)
Parke-Davis Pharmaceutical Research
Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.EBI
J Med Chem 41: 1011-3 (1998)
Merck Research Laboratories
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.BDB
Eur J Pharmacol 340: 249-58 (1997)
Mayo Clinic
Differential agonist inhibition identifies multiple epibatidine binding sites in mouse brain.BDB
J Pharmacol Exp Ther 285: 377-86 (1998)
University of Colorado
Pharmacological characterization of the human ionotropic glutamate receptor subtype GluR3 stably expressed in mammalian cells.BDB
J Pharmacol Exp Ther 285: 358-70 (1998)
SIBIA Neurosciences Inc
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach.BDB
J Pharmacol Exp Ther 285: 170-7 (1998)
University of Bonn
Synthesis and pharmacological evaluation of ring-methylated derivatives of 3,4-(methylenedioxy)amphetamine (MDA).EBI
J Med Chem 41: 1001-5 (1998)
Purdue University
Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase.EBI
J Med Chem 41: 996-1000 (1998)
G.D. Searle and Co.
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.EBI
J Med Chem 41: 913-8 (1998)
Harvard Medical School
Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.EBI
J Med Chem 41: 902-12 (1998)
University of Maryland
Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.EBI
J Med Chem 41: 877-93 (1998)
Schering-Plough Research Institute
(-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake.EBI
J Med Chem 41: 864-76 (1998)
University of Maryland
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.EBI
J Med Chem 41: 836-52 (1998)
Universidad de Alcal£
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.EBI
J Med Chem 41: 821-35 (1998)
SmithKline Beecham Pharmaceuticals
(E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists.EBI
J Med Chem 41: 808-20 (1998)
Università degli Studi di Urbino
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 2. Crystallographic and molecular modeling study of complexes of 4-amino-4H-pyran-6-carboxamides and sialidase from influenza virus types A and B.EBI
J Med Chem 41: 798-807 (1998)
Glaxo Wellcome Research and Development Limited
Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides.BDB
J Med Chem 41: 787-97 (1998)
Glaxo Wellcome Research and Development Limited
Acetamidine lysine derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide dihydrochloride: a highly selective inhibitor of human inducible nitric oxide synthase.EBI
J Med Chem 41: 775-7 (1998)
Searle
A novel kainate receptor ligand [3H]-(2S,4R)-4-methylglutamate: pharmacological characterization in rabbit brain membranes.BDB
Neuropharmacology 36: 1483-8 (1997)
University of Bristol
Discovery of nonsteroidal androgens.BDB
Biochem Biophys Res Commun 244: 1-4 (1998)
University of Tennessee at Memphis
Glyphosate is an inhibitor of plant cytochrome P450: functional expression of Thlaspi arvensae cytochrome P45071B1/reductase fusion protein in Escherichia coli.EBI
Biochem Biophys Res Commun 244: 110-4 (1998)
University of Wales Aberystwyth
Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp.EBI
J Nat Prod 61: 301-5 (1998)
Institut für Biowissenschaften
Aminopyrimidines with high affinity for both serotonin and dopamine receptors.EBI
J Med Chem 41: 760-71 (1998)
Warner-Lambert Company
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.BDB
J Med Chem 41: 742-51 (1998)
University of Auckland
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.EBI
J Med Chem 41: 728-41 (1998)
Universit£ di Siena
Potent and selective ligands for the dopamine transporter (DAT): structure-activity relationship studies of novel 4-[2-(diphenylmethoxy)ethyl]-1-(3-phenylpropyl)piperidine analogues.EBI
J Med Chem 41: 699-705 (1998)
Organix Inc
alpha-Substituted malonester amides: tools to define the relationship between ACAT inhibition and adrenal toxicity.EBI
J Med Chem 41: 682-90 (1998)
Warner-Lambert Company
Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling.EBI
J Med Chem 41: 674-81 (1998)
Universit£ degli Studi di Milano
Novel 3-aralkyl-7-(amino-substituted)-1,2,3-triazolo[4,5-d]pyrimidines with high affinity toward A1 adenosine receptors.EBI
J Med Chem 41: 668-73 (1998)
Università di Pisa
(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist.BDB
J Med Chem 41: 655-7 (1998)
SmithKline Beecham Pharmaceuticals Ltd
Carrier-mediated mechanism for the biliary excretion of the quinolone antibiotic grepafloxacin and its glucuronide in rats.EBI
J Pharmacol Exp Ther 284: 1033-9 (1998)
University of Tokyo
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.EBI
J Med Chem 41: 640-9 (1998)
Shionogi & Co., Ltd
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.EBI
J Med Chem 41: 623-39 (1998)
Ligand Pharmaceuticals Inc
Synthesis of a methylenebis(phosphonate) analogue of mycophenolic adenine dinucleotide: a glucuronidation-resistant MAD analogue of NAD.EBI
J Med Chem 41: 618-22 (1998)
Codon Pharmaceuticals, Inc.
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.EBI
J Med Chem 41: 602-17 (1998)
Abbott Laboratories
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 1. Construction of the basic framework.EBI
J Med Chem 41: 564-78 (1998)
Fujisawa Pharmaceutical Co., Ltd
A1 adenosine receptor antagonists as ligands for positron emission tomography (PET) and single-photon emission tomography (SPET).EBI
J Med Chem 41: 555-63 (1998)
Forschungszentrum Jülich GmbH
29-Methylidene-2,3-oxidosqualene derivatives as stereospecific mechanism-based inhibitors of liver and yeast oxidosqualene cyclase.EBI
J Med Chem 41: 540-54 (1998)
Università di Torino
Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitro or nitroso)pyrimidine derivatives and analogues.EBI
J Med Chem 41: 503-8 (1998)
Nagoya City University
Novel non-peptide fibrinogen receptor antagonists. 1. Synthesis and glycoprotein IIb-IIIa antagonistic activities of 1,3,4-trisubstituted 2-oxopiperazine derivatives incorporating side-chain functions of the RGDF peptide.EBI
J Med Chem 41: 489-502 (1998)
Takeda Chemical Industries, Ltd
Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors.EBI
J Med Chem 41: 468-77 (1998)
University of Illinois at Chicago
Mapping the melatonin receptor. 5. Melatonin agonists and antagonists derived from tetrahydrocyclopent[b]indoles, tetrahydrocarbazoles and hexahydrocyclohept[b]indoles.EBI
J Med Chem 41: 451-67 (1998)
University College London
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.EBI
J Med Chem 41: 437-50 (1998)
Collegeville
Specificity of diastereomers of [99mTc]TRODAT-1 as dopamine transporter imaging agents.EBI
J Med Chem 41: 428-36 (1998)
University of Pennsylvania
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.EBI
J Med Chem 41: 420-7 (1998)
OXIS International, Inc.
2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry.EBI
J Med Chem 41: 413-9 (1998)
Signal Pharmaceuticals, Inc.
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.EBI
J Med Chem 41: 407-12 (1998)
Abbott Laboratories
Ethylene biosynthesis: processing of a substrate analog supports a radical mechanism for the ethylene-forming enzyme.BDB
Chem Biol 5: 49-57 (1998)
Duke University
Engineering novel specificities for ligand-activated transcription in the nuclear hormone receptor RXR.BDB
Chem Biol 5: 13-21 (1998)
University of Texas Southwestern Medical Center
Design of potent selective zinc-mediated serine protease inhibitors.BDB
Nature 391: 608-12 (1998)
Arris
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.EBI
J Med Chem 41: 401-6 (1998)
Merck Research Laboratories
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.EBI
J Med Chem 41: 379-92 (1998)
Eli Lilly and Company
2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.EBI
J Med Chem 41: 358-78 (1998)
Eli Lilly and Company
2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution.EBI
J Med Chem 41: 346-57 (1998)
Eli Lilly and Company
Design and synthesis of malonic acid-based inhibitors of human neutrophil collagenase (MMP8).EBI
J Med Chem 41: 339-45 (1998)
Institut für Biochemie
5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists.EBI
J Med Chem 41: 311-7 (1998)
Universit£ Louis Pasteur
5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.EBI
J Med Chem 41: 303-10 (1998)
Ligand Pharmaceuticals Inc
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.EBI
J Med Chem 41: 291-302 (1998)
Ligand Pharmaceuticals Inc
Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.EBI
J Med Chem 41: 271-5 (1998)
Bristol-Myers Squibb Pharmaceutical Research Institute
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.EBI
J Med Chem 41: 266-70 (1998)
Pfizer Inc
Novel potent nonpeptide aminopeptidase N inhibitors with a cyclic imide skeleton.EBI
J Med Chem 41: 263-5 (1998)
University of Tokyo
In vitro binding characteristics of a new selective group II metabotropic glutamate receptor radioligand, [3H]LY354740, in rat brain.BDB
Mol Pharmacol 53: 228-33 (1998)
F. Hoffmann-La Roche Inc
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.BDB
Mol Pharmacol 53: 195-201 (1998)
Suntory Institute for Bioorganic Research
A new flavonol glycoside gallate ester from Acer okamotoanum and its inhibitory activity against human immunodeficiency virus-1 (HIV-1) integrase.EBI
J Nat Prod 61: 145-8 (1998)
Korea Institute of Science & Technology
Lignans interfering with 5 alpha-dihydrotestosterone binding to human sex hormone-binding globulin.EBI
J Nat Prod 61: 119-21 (1998)
Universit£t Bayreuth
Friedelane triterpenoids from Maytenus macrocarpa.EBI
J Nat Prod 61: 82-5 (1998)
Universidad de Laguna
Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers.EBI
J Nat Prod 61: 71-6 (1998)
University of Antwerp
Litebamine N-homologues: preparation and anti-acetylcholinesterase activity.EBI
J Nat Prod 61: 46-50 (1998)
National Taiwan University
Two new isoflavones from Ceiba pentandra and their effect on cyclooxygenase-catalyzed prostaglandin biosynthesis.EBI
J Nat Prod 61: 8-12 (1998)
Uppsala University
Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis.EBI
J Nat Prod 61: 2-7 (1998)
Uppsala University
Evidence for the absolute conformational specificity of the intestinal H+/peptide symporter, PEPT1.EBI
J Biol Chem 273: 3861-4 (1998)
Martin-Luther-University Halle-Wittenberg
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.BDB
Naunyn Schmiedebergs Arch Pharmacol 357: 17-24 (1998)
Eli Lilly and Company
Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.BDB
Naunyn Schmiedebergs Arch Pharmacol 357: 1-9 (1998)
Universität Würzburg
Adenosine receptor agonists: synthesis and biological evaluation of the diastereoisomers of 2-(3-hydroxy-3-phenyl-1-propyn-1-yl)NECA.BDB
Bioorg Med Chem 5: 2267-75 (1997)
Università di Camerino
Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter.EBI
Am J Physiol 274: 157-69 (1998)
Wake Forest University
Synthesis and ligand binding of tropane ring analogues of paroxetine.EBI
J Med Chem 41: 247-57 (1998)
Research Triangle Institute
Matrix metalloproteinase inhibitors: a structure-activity study.EBI
J Med Chem 41: 199-223 (1998)
Glycomed, Inc.
Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors.EBI
J Med Chem 41: 183-90 (1998)
National Institute of Diabetes
Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands.EBI
J Med Chem 41: 157-66 (1998)
University of Pennsylvania
Phenothiazine inhibitors of trypanothione reductase as potential antitrypanosomal and antileishmanial drugs.EBI
J Med Chem 41: 148-56 (1998)
University of Manchester
A new class of highly potent farnesyl diphosphate-competitive inhibitors of farnesyltransferase.EBI
J Med Chem 41: 143-7 (1998)
Tsukuba Research Institute
Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.BDB
J Pharmacol Exp Ther 284: 777-89 (1998)
SIBIA Neurosciences Inc
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.BDB
J Pharmacol Exp Ther 284: 644-50 (1998)
Sanofi Recherche
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.BDB
J Pharmacol Exp Ther 284: 500-7 (1998)
University of Arizona
Characterization of central- and peripheral-type benzodiazepine receptors in rat salivary glands.BDB
Biochem Pharmacol 55: 209-14 (1998)
Tokyo Dental College
From micromolar to nanomolar affinity: a systematic approach to identify the binding site of CGRP at the human calcitonin gene-related peptide 1 receptor.EBI
J Med Chem 41: 117-23 (1998)
ETH Zürich
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.EBI
J Med Chem 41: 109-16 (1998)
Novo Nordisk A/S
5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor.EBI
J Med Chem 41: 102-8 (1998)
Leiden/Amsterdam Center for Drug Research
Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms.EBI
J Med Chem 41: 96-101 (1998)
G. D. Searle Research and Development
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.EBI
J Med Chem 41: 74-95 (1998)
Abbott Laboratories
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.EBI
J Med Chem 41: 53-62 (1998)
DuPont Pharmaceuticals Company
Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis model.EBI
J Med Chem 41: 46-52 (1998)
National Institute of Diabetes
Second generation"peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.EBI
J Med Chem 41: 38-45 (1998)
Warner-Lambert Company
(Z)- and (E)-2-((hydroxymethyl)cyclopropylidene)methyladenine and -guanine. New nucleoside analogues with a broad-spectrum antiviral activity.EBI
J Med Chem 41: 10-23 (1998)
Wayne State University School of Medicine
2-(1-Naphthyloxy)ethylamines with enhanced affinity for human 5-HT1D beta (h5-HT1B) serotonin receptors.EBI
J Med Chem 40: 4415-9 (1998)
Medical College of Virginia/Virginia Commonwealth University
Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives.EBI
J Med Chem 40: 4406-14 (1998)
University of New Orleans
Synthesis and structure-activity relationships of 3,7-dimethyl-1-propargylxanthine derivatives, A2A-selective adenosine receptor antagonists.EBI
J Med Chem 40: 4396-405 (1998)
Julius-Maximilians-Universität Würzburg
Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase.EBI
J Med Chem 40: 4378-85 (1998)
F. Hoffmann-La Roche Inc
Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors.EBI
J Med Chem 40: 4372-7 (1998)
Schering-Plough Research Institute
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.EBI
J Med Chem 40: 4360-71 (1998)
Harvard University
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.EBI
J Med Chem 40: 4340-46 (1998)
National Institute on Drug Abuse-Intramural Research Program
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.EBI
J Med Chem 40: 4329-39 (1998)
National Institute on Drug Abuse
Fibrinogen receptor (GPIIb-IIIa) antagonists derived from 5,6-bicyclic templates. Amidinoindoles, amidinoindazoles, and amidinobenzofurans containing the N-alpha-sulfonamide carboxylic acid function as potent platelet aggregation inhibitors.EBI
J Med Chem 40: 4308-18 (1998)
COR Therapeutics Inc
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.EBI
J Med Chem 40: 4302-7 (1998)
Rochester
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compounds.EBI
J Med Chem 40: 4290-301 (1998)
Schering-Plough Research Institute
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.EBI
J Med Chem 40: 4281-9 (1998)
Cambridge NeuroScience Inc
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.EBI
J Med Chem 40: 4265-80 (1998)
SmithKline Beecham Pharmaceuticals Ltd
A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.EBI
J Med Chem 40: 4257-64 (1998)
Université d'Orléans
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.EBI
J Med Chem 40: 4235-56 (1998)
Wyeth-Ayerst Research Laboratories
Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.EBI
J Med Chem 40: 4222-34 (1998)
University of Tokyo
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles.EBI
J Med Chem 40: 4199-207 (1998)
National Cancer Institute-Frederick
Development of a high-affinity ligand that binds irreversibly to Mel1b melatonin receptors.EBI
J Med Chem 40: 4195-8 (1998)
Duquesne University
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.EBI
J Med Chem 40: 4169-94 (1998)
Abbott Laboratories
Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.BDB
Neuropsychopharmacology 18: 63-101 (1998)
H. Lundbeck A/S
Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.BDB
Science 279: 77-81 (1998)
Abbott Laboratories
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.EBI
J Med Chem 40: 4146-53 (1998)
University of Groningen
Assessment of solvation effects on calculated binding affinity differences: trypsin inhibition by flavonoids as a model system for congeneric series.EBI
J Med Chem 40: 4136-45 (1998)
Universidad de Alcalá
Peptidomimetic inhibitors of the human cytomegalovirus protease.EBI
J Med Chem 40: 4113-35 (1998)
Boehringer Ingelheim Ltd.
Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.EBI
J Med Chem 40: 4103-12 (1998)
Schering-Plough Research Institute
A strategy for the incorporation of water molecules present in a ligand binding site into a three-dimensional quantitative structure--activity relationship analysis.EBI
J Med Chem 40: 4089-102 (1998)
University of Alcala
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.EBI
J Med Chem 40: 4079-88 (1998)
DuPont Pharmaceuticals Company
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design.BDB
J Med Chem 40: 4030-52 (1997)
BioCryst Pharmaceuticals Inc
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.EBI
J Med Chem 40: 4026-9 (1998)
Warner-Lambert Company
1-[1-2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) yields two active primary metabolites in vitro: synthesis, identification from rat liver microsome extracts, and affinity for the neuronal dopamine transporter.EBI
J Med Chem 40: 4019-25 (1998)
University of Montpellier
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.EBI
J Med Chem 40: 3997-4005 (1998)
University of Kansas
Cloning and expressional characterization of a novel galanin receptor. Identification of different pharmacophores within galanin for the three galanin receptor subtypes.BDB
J Biol Chem 272: 31949-52 (1997)
Schering-Plough Research Institute
Energetics of heme binding to native and denatured states of cytochrome b562.BDB
Biochemistry 36: 16141-6 (1997)
University of Illinois
Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.BDB
J Pharmacol Exp Ther 283: 1305-22 (1997)
Emory University
Interactions of nonsteroidal anti-inflammatory drugs with rat renal organic anion transporter, OAT-K1.EBI
J Pharmacol Exp Ther 283: 1039-42 (1998)
Kyoto University Hospital
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease.EBI
J Med Chem 40: 3979-85 (1998)
Agouron Pharmaceuticals Inc
5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.EBI
J Med Chem 40: 3974-8 (1998)
Centre de Recherche Pierre Fabre
Enzymatic properties of the unnatural beta-L-enantiomers of 2',3'-dideoxyadenosine and 2',3'-didehydro-2',3'-dideoxyadenosine.EBI
J Med Chem 40: 3969-73 (1998)
University of Montpellier
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.EBI
J Med Chem 40: 3957-62 (1998)
University of Arizona
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.EBI
J Med Chem 40: 3947-56 (1998)
University of Paris
Tyrosine kinase inhibitors. 13. Structure-activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.BDB
J Med Chem 40: 3915-25 (1997)
University of Auckland
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.EBI
J Med Chem 40: 3905-14 (1998)
University of Minnesota
Potent and selective inhibition of neuronal nitric oxide synthase by N omega-propyl-L-arginine.EBI
J Med Chem 40: 3869-70 (1998)
Northwestern University
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.EBI
J Med Chem 40: 3865-8 (1998)
Merck Research Laboratories
3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter.EBI
J Med Chem 40: 3861-4 (1998)
Research Triangle Institute
Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human gamma-aminobutyric acid type A receptors.BDB
Mol Pharmacol 52: 1150-6 (1997)
Merck Sharp and Dohme Research Laboratories
Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.BDB
Life Sci 61: 2117-26 (1997)
Eli Lilly and Company
Zanhasaponins A and B, antiphospholipase A2 saponins from an antiinflammatory extract of Zanha africana root bark.EBI
J Nat Prod 60: 1158-60 (1998)
Universitat de Val£ncia
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.BDB
Chem Biol 2: 601-8 (1995)
University of California San Diego
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.BDB
Chem Biol 2: 471-81 (1995)
SmithKline Beecham Pharmaceuticals Ltd
Importance of the C-1 substituent in classical cannabinoids to CB2 receptor selectivity: synthesis and characterization of a series of O,2-propano-delta 8-tetrahydrocannabinol analogs.EBI
J Med Chem 40: 3312-8 (1997)
Kennesaw State University
17-Imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives. Novel steroidal inhibitors of human cytochrome C17,20-lyase (P450(17 alpha).EBI
J Med Chem 40: 3297-304 (1997)
University of Maryland
DNA gyrase inhibitory and antimicrobial activities of some diphenic acid monohydroxamides.EBI
J Med Chem 40: 3292-6 (1997)
R.W. Johnson Pharmaceutical Research Institute
Angiotensin analogues palmitoylated in positions 1 and 4.EBI
J Med Chem 40: 3271-9 (1997)
Universit£ de Sherbrooke
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.EBI
J Med Chem 40: 3263-70 (1997)
University of Minnesota
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.EBI
J Med Chem 40: 3248-53 (1997)
Hokuriku University
Sulfated galactocerebrosides as potential antiinflammatory agents.EBI
J Med Chem 40: 3234-47 (1997)
Bristol-Myers Squibb Pharmaceutical Research Institute
Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.EBI
J Med Chem 40: 3228-33 (1997)
Institute of Science
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.EBI
J Med Chem 40: 3217-27 (1997)
Abbott Laboratories
A model for binding of structurally diverse natural product inhibitors of protein phosphatases PP1 and PP2A.EBI
J Med Chem 40: 3199-206 (1997)
University of California
Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.EBI
J Med Chem 40: 3192-8 (1997)
SmithKline Beecham S.p.A.
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.EBI
J Med Chem 40: 3173-81 (1997)
Zeneca Pharmaceuticals
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.EBI
J Med Chem 40: 3161-72 (1997)
University of Michigan
NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.EBI
J Med Chem 40: 3144-50 (1997)
Abbott Laboratories
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prEBI
J Med Chem 40: 3141-3 (1997)
Abbott Laboratories
Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells.EBI
Am J Physiol 273: 706-11 (1997)
Kyoto University Hospital
Design, synthesis, and biochemical evaluation of phosphonate and phosphonamidate analogs of glutathionylspermidine as inhibitors of glutathionylspermidine synthetase/amidase from Escherichia coli.EBI
J Med Chem 40: 3842-50 (1997)
University of Michigan
Synthesis and structure-activity profiles of A-homoestranes, the estratropones.EBI
J Med Chem 40: 3836-41 (1997)
University of Virginia
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.EBI
J Med Chem 40: 3804-19 (1997)
Uppsala University
4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.BDB
J Med Chem 40: 3781-92 (1997)
Parke-Davis Pharmaceutical Research
Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity.EBI
J Med Chem 40: 3773-80 (1997)
Westfälische Wilhelms-Universität Münster
N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists.EBI
J Med Chem 40: 3765-72 (1997)
University of Ghent
Synthesis and biological evaluation of 4-(hydroxyalkyl)estradiols and related compounds.EBI
J Med Chem 40: 3756-64 (1997)
Ohio State University
Betidamino acid scan of the GnRH antagonist acyline.EBI
J Med Chem 40: 3739-48 (1997)
Salk Institute
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.EBI
J Med Chem 40: 3726-33 (1997)
Merck Research Laboratories
Design, synthesis, and cocrystal structure of a nonpeptide Src SH2 domain ligand.EBI
J Med Chem 40: 3719-25 (1997)
Warner-Lambert Company
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.EBI
J Med Chem 40: 3712-4 (1997)
Eli Lilly and Company
Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: the profound effect of polarity on antiviral activity.BDB
J Med Chem 40: 3707-11 (1997)
Parke-Davis Pharmaceutical Research
(S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors.EBI
J Med Chem 40: 3700-5 (1997)
Royal Danish School of Pharmacy
2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.EBI
J Med Chem 40: 3694-9 (1997)
Harvard Medical School
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.EBI
J Med Chem 40: 3687-93 (1997)
Merck Research Laboratories
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.EBI
J Med Chem 40: 3679-86 (1997)
CoCensys Inc
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.EBI
J Med Chem 40: 3670-8 (1997)
Universit£ di Siena
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.EBI
J Med Chem 40: 3645-50 (1997)
University of Bristol
Synthesis and pharmacological comparison of dimethylheptyl and pentyl analogs of anandamide.EBI
J Med Chem 40: 3626-34 (1997)
Research Triangle Institute
Potent anandamide analogs: the effect of changing the length and branching of the end pentyl chain.EBI
J Med Chem 40: 3617-25 (1997)
Organix Inc
Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.BDB
J Med Chem 40: 3601-16 (1997)
Novartis Pharmaceuticals
Design, synthesis, and dopamine receptor modulating activity of diketopiperazine peptidomimetics of L-prolyl-L-leucylglycinamide.EBI
J Med Chem 40: 3594-600 (1997)
University of Minnesota
Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain.EBI
J Med Chem 40: 3551-6 (1997)
Novartis Pharma Inc
Differentiation between partial agonists and neutral 5-HT1B antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562).EBI
J Med Chem 40: 3542-50 (1997)
Centre de Recherche Pierre Fabre
Studies on selection blockers. 5. Design, synthesis, and biological profile of sialyl Lewis x mimetics based on modified serine-glutamic acid dipeptides.EBI
J Med Chem 40: 3534-41 (1997)
Kanebo
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.EBI
J Med Chem 40: 3524-33 (1997)
Universit£t Regensburg
Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors.EBI
J Med Chem 40: 3516-23 (1997)
University of Strathclyde
Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.EBI
J Med Chem 40: 3504-7 (1997)
Shionogi & Co., Ltd
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.EBI
J Med Chem 40: 3501-3 (1997)
Merck Sharp and Dohme Research Laboratories
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.EBI
J Med Chem 40: 3497-500 (1997)
Merck Sharp and Dohme Research Laboratories
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.EBI
J Med Chem 40: 3494-6 (1997)
SmithKline Beecham Pharmaceuticals Ltd
ATP-dependent transport of bilirubin glucuronides by the multidrug resistance protein MRP1 and its hepatocyte canalicular isoform MRP2.EBI
Biochem J 327: 305-10 (1997)
Deutsches Krebsforschungszentrum
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.BDB
J Pharmacol Exp Ther 283: 735-41 (1997)
Torrey Pines Institute for Molecular Studies
[3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits.BDB
J Pharmacol Exp Ther 283: 488-93 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.BDB
Neuroreport 8: 3189-96 (1997)
CNRS UPR 9023
Cloning and expression of a human serotonin 5-HT4 receptor cDNA.BDB
J Neurochem 69: 1810-9 (1997)
Janssen Research Foundation
Synthesis, cardiotonic activity, and structure-activity relationships of 17 beta-guanylhydrazone derivatives of 5 beta-androstane-3 beta, 14 beta-diol acting on the Na+,K(+)-ATPase receptor.EBI
J Med Chem 40: 3484-8 (1997)
Prassis Istituto di Ricerche Sigma-Tau
Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group.EBI
J Med Chem 40: 3456-65 (1997)
Université Blaise Pascal
Thromboxane modulating agents. 3. 1H-imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists.EBI
J Med Chem 40: 3442-52 (1997)
Pfizer Inc
7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase.EBI
J Med Chem 40: 3423-33 (1997)
Southern Methodist University
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.EBI
J Med Chem 40: 3408-22 (1997)
Rhône-Poulenc Rorer
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.EBI
J Med Chem 40: 3402-7 (1997)
Instituto de Química Médica (CSIC)
New orally active non-peptide fibrinogen receptor (GpIIb-IIIa) antagonists: identification of ethyl 3-[N-[4-[4-[amino[(ethoxycarbonyl) imino]methyl]phenyl]-1,3-thiazol-2-yl]-N-[1-[(ethoxycarbonyl)methyl]pip erid -4-yl]amino]propionate (SR 121787) as a potent and long-acting antithrombotic agent.EBI
J Med Chem 40: 3393-401 (1997)
Sanofi Recherche
Structure-activity relationships of (4-acylpyrrol-2-yl)alkanoic acids as inhibitors of the cytosolic phospholipase A2: variation of the substituents in positions 1, 3, and 5.EBI
J Med Chem 40: 3381-92 (1997)
Ludwig-Maximilians University
Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.EBI
J Med Chem 40: 3369-80 (1997)
Pharmacia & Upjohn
Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.EBI
J Med Chem 40: 3359-68 (1997)
Genentech Inc
Effect of a chemical modification on the hydrated adenosine intermediate produced by adenosine deaminase and a model reaction for a potential mechanism of action of 5-aminoimidazole ribonucleotide carboxylase.EBI
J Med Chem 40: 3336-45 (1997)
Southern Illinois University
C-terminal modifications of histidyl-N-benzylglycinamides to give improved inhibition of Ras farnesyltransferase, cellular activity, and anticancer activity in mice.EBI
J Med Chem 40: 3319-22 (1997)
Warner-Lambert Company
The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.BDB
J Pharmacol Exp Ther 283: 216-25 (1997)
Preclinical R & D, Astra Arcus AB
Four new clerodane diterpenes from the leaves of Casearia guianensis which inhibit the interaction of leukocyte function antigen 1 with intercellular adhesion molecule 1.EBI
J Nat Prod 60: 894-9 (1997)
Searle Research and Development
In vitro anti-HIV activity of biflavonoids isolated from Rhus succedanea and Garcinia multiflora.EBI
J Nat Prod 60: 884-8 (1997)
MediChem Research, Inc.
Biliary excretion of pravastatin in rats: contribution of the excretion pathway mediated by canalicular multispecific organic anion transporter.EBI
Drug Metab Dispos 25: 1123-9 (1997)
Toho University School of Pharmaceutical Sciences
Interaction of cyclosporin derivatives with the ATPase activity of human P-glycoprotein.EBI
Br J Pharmacol 122: 241-8 (1997)
Novartis Takarazuka Research Institute
Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.BDB
Br J Pharmacol 122: 217-24 (1997)
Kyoto University
Expression cloning of a rat hypothalamic galanin receptor coupled to phosphoinositide turnover.BDB
J Biol Chem 272: 24612-6 (1997)
Synaptic Pharmaceutical Corporation
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.BDB
Naunyn Schmiedebergs Arch Pharmacol 356: 328-34 (1997)
Rhône-Poulenc Rorer
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 356: 312-20 (1997)
SmithKline Beecham Pharmaceuticals Ltd
Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants.BDB
FEBS Lett 413: 489-94 (1997)
Organon N.V.
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.EBI
J Med Chem 40: 3119-29 (1997)
Université René Descartes-Paris V
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.EBI
J Med Chem 40: 3109-18 (1997)
Universit£ degli Studi di Bari
Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.EBI
J Med Chem 40: 3100-8 (1997)
University of Ferrara
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.EBI
J Med Chem 40: 3091-9 (1997)
Klinikum der Friedrich-Schiller-Universit£t Jena
Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.EBI
J Med Chem 40: 3085-90 (1997)
Chinese Academy of Sciences
7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.EBI
J Med Chem 40: 3064-70 (1997)
University of Minnesota
Curcumin analogs with altered potencies against HIV-1 integrase as probes for biochemical mechanisms of drug action.EBI
J Med Chem 40: 3057-63 (1997)
National Cancer Institute-Bethesda
Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.EBI
J Med Chem 40: 3049-56 (1997)
University of North Carolina
Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.EBI
J Med Chem 40: 3040-8 (1997)
University
Conformationally restricted analogues of trimethoprim: 2,6-diamino-8-substituted purines as potential dihydrofolate reductase inhibitors from Pneumocystis carinii and Toxoplasma gondii.EBI
J Med Chem 40: 3032-9 (1997)
Duquesne University
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".EBI
J Med Chem 40: 3014-24 (1997)
University of Tennessee
Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase.EBI
J Med Chem 40: 3009-13 (1997)
University of North Texas
Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives.EBI
J Med Chem 40: 2997-3008 (1997)
Purdue University
Fused pyrrolo[2,3-c]carbazol-6-ones: novel immunostimulants that enhance human interferon-gamma activity.EBI
J Med Chem 40: 2994-6 (1997)
Cephalon, Inc.
Ras farnesyltransferase: a new therapeutic target.EBI
J Med Chem 40: 2971-90 (1997)
Warner-Lambert Company
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).BDB
Br J Pharmacol 122: 126-32 (1997)
Roche Bioscience
The somatostatin analog octreotide as potential treatment for re-stenosis and chronic rejection.BDB
Transplant Proc 29: 2599-600 (1997)
Novartis Pharma Research
Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.EBI
J Med Chem 40: 2948-52 (1997)
University of Ferrara
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.EBI
J Med Chem 40: 2936-47 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as antagonists of the NMDA receptor-channel complex.EBI
J Med Chem 40: 2922-30 (1997)
TBA
Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide (PK11195).EBI
J Med Chem 40: 2910-21 (1997)
Universit£ di Siena
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.EBI
J Med Chem 40: 2895-901 (1997)
National Institute on Aging
Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.EBI
J Med Chem 40: 2866-75 (1997)
Merck Frosst Centre for Therapeutic Research
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists.EBI
J Med Chem 40: 2843-57 (1997)
Eli Lilly and Company
Selective inhibition of neuronal nitric oxide synthase by N omega-nitroarginine-and phenylalanine-containing dipeptides and dipeptide esters.EBI
J Med Chem 40: 2813-7 (1997)
Northwestern University
Structure and anti-acetylcholinesterase activity of 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B.EBI
J Nat Prod 60: 842-3 (1997)
National Taiwan University
Molecular cloning and pharmacological characterization of a new galanin receptor subtype.BDB
Mol Pharmacol 52: 337-43 (1997)
The Schering Plough Research Institute
Antipsoriatic anthrones with modulated redox properties. 4. Synthesis and biological activity of novel 9,10-dihydro-1,8-dihydroxy-9-oxo-2-anthracenecarboxylic and -hydroxamic acids.EBI
J Med Chem 40: 2780-7 (1997)
Westfälische Wilhelms-Universität Münster
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.EBI
J Med Chem 40: 2762-9 (1997)
F. Hoffmann-La Roche Inc
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.EBI
J Med Chem 40: 2740-9 (1997)
University of Arizona
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.EBI
J Med Chem 40: 2733-9 (1997)
Oregon State University
Synthesis and antimalarial effects of phenothiazine inhibitors of a Plasmodium falciparum cysteine protease.EBI
J Med Chem 40: 2726-32 (1997)
Universidad Central de Venezuela
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.BDB
J Med Chem 40: 2706-25 (1997)
Glaxo Wellcome Research and Development
Synthesis, biological evaluation, and structure-activity relationships of 3-acylindole-2-carboxylic acids as inhibitors of the cytosolic phospholipase A2.EBI
J Med Chem 40: 2694-705 (1997)
Ludwig-Maximilians University
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.EBI
J Med Chem 40: 2688-93 (1997)
Warner-Lambert Company
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.EBI
J Med Chem 40: 2674-87 (1997)
Roche Bioscience
2-Carbomethoxy-3-aryl-8-oxabicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.EBI
J Med Chem 40: 2661-73 (1997)
Organix Inc
Methotrexate is excreted into the bile by canalicular multispecific organic anion transporter in rats.EBI
Cancer Res 57: 3506-10 (1997)
Toho University School of Pharmaceutical Sciences
I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor.BDB
J Pharmacol Exp Ther 282: 1011-9 (1997)
Neurogen Corporation
Kinetic analysis of the primary active transport of conjugated metabolites across the bile canalicular membrane: comparative study of S-(2,4-dinitrophenyl)-glutathione and 6-hydroxy-5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl)benzothiazole glucuronide.EBI
J Pharmacol Exp Ther 282: 866-72 (1997)
University of Tokyo
Cloning and characterization of two human polyspecific organic cation transporters.EBI
DNA Cell Biol 16: 871-81 (1997)
Anatomisches Institut der Bayerischen Julius-Maximilians-Universit£t
Synthesis and structure-activity relationships of a new model of arylpiperazines. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity.EBI
J Med Chem 40: 2653-6 (1997)
Universidad Complutense
Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.EBI
J Med Chem 40: 2609-25 (1997)
G.D. Searle and Company
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.EBI
J Med Chem 40: 2596-608 (1997)
National Institute of Diabetes
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.EBI
J Med Chem 40: 2588-95 (1997)
NIDDK
Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.EBI
J Med Chem 40: 2579-87 (1997)
National Institute of Environmental Health Sciences
H3-receptor antagonists: synthesis and structure-activity relationships of para- and meta-substituted 4(5)-phenyl-2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazoles.EBI
J Med Chem 40: 2571-8 (1997)
Universit£ degli Studi di Parma
The chemistry of pseudomonic acid. 18. Heterocyclic replacement of the alpha,beta-unsaturated ester: synthesis, molecular modeling, and antibacterial activity.EBI
J Med Chem 40: 2563-70 (1997)
SmithKline Beecham Pharmaceuticals Ltd
The role of phenylalanine at position 6 in glucagon's mechanism of biological action: multiple replacement analogues of glucagon.EBI
J Med Chem 40: 2555-62 (1997)
University of Arizona
Synthesis of nonhydrolyzable analogues of thiazole-4-carboxamide and benzamide adenine dinucleotide containing fluorine atom at the C2' of adenine nucleoside: induction of K562 differentiation and inosine monophosphate dehydrogenase inhibitory activity.EBI
J Med Chem 40: 2533-8 (1997)
Codon Pharmaceuticals, Inc.
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.BDB
J Med Chem 40: 2525-32 (1997)
Novartis Pharmaceuticals
Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition.EBI
J Med Chem 40: 2502-24 (1997)
Agouron Pharmaceuticals Inc
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.EBI
J Med Chem 40: 2491-501 (1997)
Merck Sharp & Dohme Research Laboratories
Synthesis and ligand binding studies of 4'-iodobenzoyl esters of tropanes and piperidines at the dopamine transporter.EBI
J Med Chem 40: 2474-81 (1997)
University of Oklahoma
Selective inhibitors of monoamine oxidase. 4. SAR of tricyclic N-methylcarboxamides and congeners binding at the tricyclics' hydrophilic binding site.EBI
J Med Chem 40: 2466-73 (1997)
Wellcome Research Laboratories
Identification of highly potent retinoic acid receptor alpha-selective antagonists.EBI
J Med Chem 40: 2445-51 (1997)
Allergan Inc
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.EBI
J Med Chem 40: 2440-4 (1997)
University of Pennsylvania
Thermodynamic and structural analysis of phosphotyrosine polypeptide binding to Grb2-SH2.BDB
Biochemistry 36: 10006-14 (1997)
Schering-Plough Research Institute
Novel selective thiol inhibitors of neutral endopeptidase containing heterocycles at P'2 position.BDB
J Enzym Inhib 12: 155-60 (1997)
R & D, Zambon Group Spa
Yeast hexokinase inhibitors designed from the 3-D enzyme structure rebuilding.BDB
J Enzym Inhib 12: 101-21 (1997)
Universite Paul Sabatier
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 6. 2-Indol-3-yl- and 2-azaindol-3-yl-dipyridodiazepinones.BDB
J Med Chem 40: 2430-3 (1997)
Boehringer Ingelheim Pharmaceuticals Inc
Synthesis of racemic 6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones as antagonists of N-methyl-d-aspartate (NMDA) and alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors.EBI
J Med Chem 40: 2424-9 (1997)
CoCensys Inc
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.EBI
J Med Chem 40: 2374-85 (1997)
Merck Sharp and Dohme Research Laboratories
Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils.EBI
J Med Chem 40: 2363-73 (1997)
Life Science Research Center
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.EBI
J Med Chem 40: 2347-62 (1997)
Monash University
Synthesis of analogs of 2-methoxyestradiol with enhanced inhibitory effects on tubulin polymerization and cancer cell growth.EBI
J Med Chem 40: 2323-34 (1997)
Purdue University
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.EBI
J Med Chem 40: 2296-303 (1997)
Parke-Davis Pharmaceutical Research
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.EBI
J Med Chem 40: 2289-92 (1997)
SmithKline Beecham Pharmaceuticals Ltd
Unsaturated phosphinic analogues of gamma-aminobutyric acid as GABA(C) receptor antagonists.BDB
Eur J Pharmacol 329: 223-9 (1997)
University of Sydney
Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.BDB
Neuropharmacology 36: 713-20 (1997)
F. Hoffmann-La Roche Inc
[3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors.BDB
Neuropharmacology 36: 671-9 (1997)
Roche Bioscience
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.BDB
Neuropharmacology 36: 621-9 (1997)
Roche Bioscience
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.BDB
Neuropharmacology 36: 609-20 (1997)
SmithKline Beecham Pharmaceuticals Ltd
Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin.BDB
Chem Biol 4: 461-71 (1997)
Massachusetts Institute of Technology
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.BDB
Chem Biol 4: 423-31 (1997)
Vertex Pharmaceuticals Inc
N-(3-lodoprop-2E-enyl)-2beta-carbomethoxy-3beta-(3',4'-dichloro phenyl)nortropane (beta-CDIT), a tropane derivative: pharmacological characterization as a specific ligand for the dopamine transporter in the rodent brain.BDB
J Pharmacol Exp Ther 282: 467-74 (1997)
University of Tours
[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors.BDB
J Pharmacol Exp Ther 282: 445-51 (1997)
Georgetown University
Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo.BDB
J Pharmacol Exp Ther 282: 301-8 (1997)
Yamanouchi Pharmaceutical Co., Ltd
[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents.BDB
J Pharmacol Exp Ther 282: 181-91 (1997)
Institut de Recherches Servier
Antitumor agents. 174. 2',3',4',5,6,7-Substituted 2-phenyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.EBI
J Med Chem 40: 2266-75 (1997)
University of North Carolina at Chapel Hill
A refined model for the somatostatin pharmacophore: conformational analysis of lanthionine-sandostatin analogs.EBI
J Med Chem 40: 2252-8 (1997)
University of California San Diego
Lanthionine-somatostatin analogs: synthesis, characterization, biological activity, and enzymatic stability studies.EBI
J Med Chem 40: 2241-51 (1997)
University of California San Diego
Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.EBI
J Med Chem 40: 2228-40 (1997)
Warner-Lambert Company
Steroidal affinity labels of the estrogen receptor. 3. Estradiol 11 beta-n-alkyl derivatives bearing a terminal electrophilic group: antiestrogenic and cytotoxic properties.EBI
J Med Chem 40: 2217-27 (1997)
INSERM Unit� 439
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.EBI
J Med Chem 40: 2196-210 (1997)
Schering-Plough Research Institute
Phosphodiester amidates of unsaturated nucleoside analogues: synthesis and anti-HIV activity.EBI
J Med Chem 40: 2191-5 (1997)
Wayne State University School of Medicine
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.BDB
J Med Chem 40: 2164-76 (1997)
Boehringer Ingelheim (Canada) Ltd
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.EBI
J Med Chem 40: 2156-63 (1997)
Suntory Ltd.
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.EBI
J Med Chem 40: 2133-9 (1997)
University of Michigan Medical Center
(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.EBI
J Med Chem 40: 2123-5 (1997)
Abbott Laboratories
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.EBI
J Med Chem 40: 2117-22 (1997)
Le Centre Hospitalier Universitaire de Qu£bec
Inhibition of human telomerase by a G-quadruplex-interactive compound.EBI
J Med Chem 40: 2113-6 (1997)
Institute for Drug Development
Activity of Parthenolide at 5HT2A receptors.EBI
J Nat Prod 60: 651-3 (1997)
University of Montana
Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis.EBI
J Nat Prod 60: 638-41 (1997)
University of Antwerp
Effects of flavonoids isolated from scutellariae radix on fibrinolytic system induced by trypsin in human umbilical vein endothelial cells.EBI
J Nat Prod 60: 598-601 (1997)
Ehime University
Non-peptide RGD surrogates which mimic a Gly-Asp beta-turn: potent antagonists of platelet glycoprotein IIb-IIIa.EBI
J Med Chem 40: 2085-101 (1997)
Eli Lilly and Company
Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists.EBI
J Med Chem 40: 2064-84 (1997)
DuPont Pharmaceuticals Company
Synthesis and in vitro evaluation of two progressive series of bifunctional polyhydroxybenzamide catechol-O-methyltransferase inhibitors.EBI
J Med Chem 40: 2035-9 (1997)
University of Otago
(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.EBI
J Med Chem 40: 2017-34 (1997)
Merck KGaA
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.EBI
J Med Chem 40: 2003-10 (1997)
Universit£ degli Studi di Urbino
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.EBI
J Med Chem 40: 1990-2002 (1997)
Universit£ degli Studi di Urbino
Probing the active sites of monoamine oxidase A and B with 1,4-disubstituted tetrahydropyridine substrates and inactivators.EBI
J Med Chem 40: 1982-9 (1997)
Virginia Polytechnic Institute and State University
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.EBI
J Med Chem 40: 1977-81 (1997)
University of Minnesota
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.EBI
J Med Chem 40: 1955-68 (1997)
Abbott Laboratories
Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1 beta-converting enzyme inhibitor.EBI
J Med Chem 40: 1941-6 (1997)
Sanofi Winthrop Inc.
Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor.BDB
Mol Pharmacol 51: 350-6 (1997)
Schering-Plough Research Institute
Molecular recognition at the thrombin active site: structure-based design and synthesis of potent and selective thrombin inhibitors and the X-ray crystal structures of two thrombin-inhibitor complexes.BDB
Chem Biol 4: 287-95 (1997)
Laboratorium für Organische Chemie
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.BDB
Chem Biol 4: 297-307 (1997)
University of California Berkeley
Synthesis and biological activities of conformationally restricted, tricyclic nonclassical antifolates as inhibitors of dihydrofolate reductases.EBI
J Med Chem 40: 1930-6 (1997)
Duquesne University
Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.EBI
J Med Chem 40: 1906-18 (1997)
Institut de Recherche Servier
Substituted N-phenylisothioureas: potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity.EBI
J Med Chem 40: 1901-5 (1997)
Glaxo Wellcome Research and Development
Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase.EBI
J Med Chem 40: 1886-93 (1997)
University of Nottingham
Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.EBI
J Med Chem 40: 1876-85 (1997)
Zeneca Pharmaceuticals
Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives.EBI
J Med Chem 40: 1863-9 (1997)
Kyowa Hakko Kogyo Co., Ltd
A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain.EBI
J Med Chem 40: 1835-44 (1997)
Organix Inc
Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.BDB
J Med Chem 40: 1820-6 (1997)
University of Auckland
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.EBI
J Med Chem 40: 1808-19 (1997)
Universit£ de Caen
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.EBI
J Med Chem 40: 1794-807 (1997)
SmithKline Beecham S.p.A. Milano
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.EBI
J Med Chem 40: 1779-88 (1997)
Merck Research Laboratories
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.EBI
J Med Chem 40: 1773-8 (1997)
CV Therapeutics
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.EBI
J Med Chem 40: 1771-2 (1997)
Warner-Lambert Company
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.EBI
J Med Chem 40: 1768-70 (1997)
UPR 421 du CNRS
Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.EBI
J Med Chem 40: 1763-7 (1997)
Centre de Recherches de Vitry-Alfortville
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.BDB
J Pharmacol Exp Ther 281: 1303-11 (1997)
SmithKline Beecham Pharmaceuticals Ltd
Anthracyclines modulate multidrug resistance protein (MRP) mediated organic anion transport.EBI
Biochim Biophys Acta 1326: 12-22 (1997)
Academic Hospital Vrije Universiteit
Cloning and functional expression of a human liver organic cation transporter.EBI
Mol Pharmacol 51: 913-21 (1997)
University of California San Francisco
Rabbit cerebral cortex 5HT1a receptors.BDB
Comp Biochem Physiol C, Pharmacol Toxicol Endocrinol 117: 19-24 (1997)
University of Montana
Perhydrogenation of tabersonine, ans Aspidiosperma indole alkaloid.EBI
J Nat Prod 60: 419-20 (1997)
Université de Caen Basse-Normandle
A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis.BDB
Nature 387: 620-4 (1997)
The University of Tokyo
Arylcarbamate derivatives of 1-piperidineethanol as potent ligands for 5-HT4 receptors.EBI
J Med Chem 40: 1755-61 (1997)
CNRS-BIOCIS
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.EBI
J Med Chem 40: 1749-54 (1997)
Pfizer Inc
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.EBI
J Med Chem 40: 1738-48 (1997)
University of Michigan Medical Center
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.EBI
J Med Chem 40: 1726-30 (1997)
University of Kansas
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.EBI
J Med Chem 40: 1720-5 (1997)
University of Minnesota
Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors.BDB
J Med Chem 40: 1707-9 (1997)
DuPont Pharmaceuticals Company
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.EBI
J Med Chem 40: 1690-7 (1997)
ImmunoPharmaceutics Inc.
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.EBI
J Med Chem 40: 1682-9 (1997)
ImmunoPharmaceutics Inc.
Halogenated 4-(phenoxymethyl)piperidines as potential radiolabeled probes for sigma-1 receptors: in vivo evaluation of [123I]-1-(iodopropen-2-yl)-4-[(4-cyanophenoxy)methyl]pip eri dine.EBI
J Med Chem 40: 1657-67 (1997)
ANSTO
Synthesis and structure-activity relationships of a new model of arylpiperazines. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparison of CoMFA models.EBI
J Med Chem 40: 1648-56 (1997)
Universidad Complutense
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents.EBI
J Med Chem 40: 1634-47 (1997)
Searle Research and Development
1,2-Diarylpyrroles as potent and selective inhibitors of cyclooxygenase-2.EBI
J Med Chem 40: 1619-33 (1997)
Searle Research and Development
Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5'-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues.EBI
J Med Chem 40: 1608-18 (1997)
Brigham Young University
Synthesis and pharmacological properties of a close analogue of an antithrombotic pentasaccharide (SR 90107A/ORG 31540).EBI
J Med Chem 40: 1600-7 (1997)
Sanofi Recherche
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.EBI
J Med Chem 40: 1585-99 (1997)
Abbott Laboratories
Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics as inhibitors of angiotensin-converting enzyme and neutral endopeptidase.EBI
J Med Chem 40: 1570-7 (1997)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.EBI
J Med Chem 40: 1565-9 (1997)
Merck Research Laboratories
Identification of the novel antimicrobial fatty acid (5Z,9Z)-14-methyl-5,9-pentadecadienoic acid in Eunicea succinea.EBI
J Nat Prod 60: 502-4 (1997)
University of Puerto Rico
Differential expression of multiple somatostatin receptors in the rat cerebellum during development.BDB
J Neurochem 68: 2263-72 (1997)
Dynamique des Systemes Neuroendocriniens
The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons.BDB
Eur J Pharmacol 325: 145-53 (1997)
CNS-Pharmacology
Fagomine isomers and glycosides from Xanthocercis zambesiaca.EBI
J Nat Prod 60: 312-4 (1997)
Hokuriku University
Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs.EBI
J Med Chem 40: 1550-8 (1997)
Institut de Chimie des Substances Naturelles CNRS
Binding affinities for sulfonamide inhibitors with human thrombin using Monte Carlo simulations with a linear response method.EBI
J Med Chem 40: 1539-49 (1997)
Yale University
Tyrosine kinase inhibitors. 11. Soluble analogues of pyrrolo- and pyrazoloquinazolines as epidermal growth factor receptor inhibitors: synthesis, biological evaluation, and modeling of the mode of binding.BDB
J Med Chem 40: 1519-29 (1997)
University of Auckland
Folate-based inhibitors of thymidylate synthase: synthesis and antitumor activity of gamma-linked sterically hindered dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).EBI
J Med Chem 40: 1495-510 (1997)
The Institute of Cancer Research
Improved P1/P1' substituents for cyclic urea based HIV-1 protease inhibitors: synthesis, structure-activity relationship, and X-ray crystal structure analysis.BDB
J Med Chem 40: 1465-74 (1997)
DuPont Pharmaceuticals Company
Smart region definition: a new way to improve the predictive ability and interpretability of three-dimensional quantitative structure-activity relationships.EBI
J Med Chem 40: 1455-64 (1997)
University of Perugia
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.BDB
J Med Chem 40: 1447-54 (1997)
Sapienza University of Rome
Synthesis and structure-activity relationships of 17beta-substituted 14beta-hydroxysteroid 3-(alpha-L-rhamnopyranoside)s: steroids that bind to the digitalis receptor.EBI
J Med Chem 40: 1439-46 (1997)
University of Manitoba
Conformationally constrained [p-(omega-aminoalkyl)phenacetyl]-L-seryl-L-lysyl dipeptide amides as potent peptidomimetic inhibitors of Candida albicans and human myristoyl-CoA:protein N-myristoyl transferase.EBI
J Med Chem 40: 1422-38 (1997)
G. D. Searle Research and Development
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.EBI
J Med Chem 40: 1417-21 (1997)
Dipartimento di Scienze Farmaceutiche, Firenze, Italy.
Novel cyclic peptide agonist of high potency and selectivity for the type II vasoactive intestinal peptide receptor.BDB
J Pharmacol Exp Ther 281: 629-33 (1997)
University of California San Francisco
The 5-HT7 receptor: orphan found.BDB
Trends Pharmacol Sci 18: 104-7 (1997)
Roche Bioscience
BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.BDB
Neuropharmacology 36: 233-9 (1997)
SmithKline Beecham Pharmaceuticals Ltd
Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.EBI
Science 276: 955-60 (1997)
New York University Medical Center
Synthesis and ligand binding of nortropane derivatives: N-substituted 2beta-carbomethoxy-3beta-(4'-iodophenyl)nortropane and N-(3-iodoprop-(2E)-enyl)-2beta-carbomethoxy-3beta-(3',4'-disubstituted phenyl)nortropane. New high-affinity and selective compounds for the dopamine transporter.EBI
J Med Chem 40: 1366-72 (1997)
University of Tours
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).EBI
J Med Chem 40: 1347-65 (1997)
Searle Research and Development
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.EBI
J Med Chem 40: 1316-26 (1997)
Georgetown University Medical Center
Pharmacological options in the treatment of benign prostatic hyperplasia.EBI
J Med Chem 40: 1293-315 (1997)
Pfizer Inc
Isolation and structure determination of sulfonoquinovosyl dipalmitoyl glyceride, a P-selectin receptor inhibitor from the alga Dictyochloris fragrans.EBI
J Nat Prod 60: 387-9 (1997)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pharmacology and functions of metabotropic glutamate receptors.BDB
Annu Rev Pharmacol Toxicol 37: 205-37 (1997)
Emory University
Identification and characterization of the leech CNS cannabinoid receptor: coupling to nitric oxide release.BDB
Brain Res 753: 219-24 (1997)
State University of New York at Old Westbury
Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy.EBI
J Med Chem 40: 1270-5 (1997)
Institute of Cancer Research
N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.EBI
J Med Chem 40: 1252-7 (1997)
Yamanouchi Pharmaceutical Company, Ltd
Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters.EBI
J Med Chem 40: 1247-51 (1997)
Research Triangle Institute
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.EBI
J Med Chem 40: 1230-46 (1997)
The University of Toledo
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.EBI
J Med Chem 40: 1211-8 (1997)
Oregon State University
Novel indole-2-carboxamide and cycloalkeno[1,2-b]indole derivatives. Structure-activity relationships for high inhibition of human LDL peroxidation.EBI
J Med Chem 40: 1201-10 (1997)
Université H. Poincaré
Arylamide inhibitors of HIV-1 integrase.EBI
J Med Chem 40: 1186-94 (1997)
National Cancer Institute-Bethesda
Molecular cloning and characterization of a new receptor for galanin.BDB
FEBS Lett 405: 285-90 (1997)
Merck Research Laboratories
PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties.BDB
J Pharmacol Exp Ther 281: 440-7 (1997)
Pharmacia & Upjohn
Multispecific organic anion transporter is responsible for the biliary excretion of the camptothecin derivative irinotecan and its metabolites in rats.EBI
J Pharmacol Exp Ther 281: 304-14 (1997)
University of Tokyo
Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2.EBI
Biochim Biophys Acta 1324: 296-308 (1997)
Medical College of Georgia
Rigidone, a sesquiterpene o-quinone from the gorgonian Pseudopterogorgia rigida.EBI
J Nat Prod 60: 309-11 (1997)
SmithKline Beecham Pharmaceuticals Ltd
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.BDB
Naunyn Schmiedebergs Arch Pharmacol 355: 365-75 (1997)
Northwestern University
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.EBI
J Med Chem 40: 1173-7 (1997)
Duquesne University
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.EBI
J Med Chem 40: 1169-72 (1997)
Abbott Laboratories
4-substituted cubylcarbinylamines: a new class of mechanism-based monoamine oxidase B inactivators.EBI
J Med Chem 40: 1165-8 (1997)
Northwestern University
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.BDB
J Med Chem 40: 1149-64 (1997)
Upjohn
Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases.EBI
J Med Chem 40: 1130-5 (1997)
Warner-Lambert Company
19-nor-10-azasteroids: a novel class of inhibitors for human steroid 5alpha-reductases 1 and 2.EBI
J Med Chem 40: 1112-29 (1997)
Universit£ di Firenze
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.EBI
J Med Chem 40: 1104-11 (1997)
Universit£ de Versailles/St. Quentin-en-Yvelines
Synthesis and structure-activity relationships of carboxylated chalcones: a novel series of CysLT1 (LTD4) receptor antagonists.EBI
J Med Chem 40: 1075-89 (1997)
Vrije Universiteit
Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.EBI
J Med Chem 40: 1063-74 (1997)
Warner-Lambert Company
Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.EBI
J Med Chem 40: 1049-62 (1997)
Abbott Laboratories
Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.EBI
J Med Chem 40: 1026-40 (1997)
Merck Research Laboratories
Structural analogues of the calanolide anti-HIV agents. Modification of the trans-10,11-dimethyldihydropyran-12-ol ring (ring C).EBI
J Med Chem 40: 1005-17 (1997)
MediChem Research, Inc.
New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.EBI
J Med Chem 40: 996-1004 (1997)
Zeneca Pharmaceuticals
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.EBI
J Med Chem 40: 990-5 (1997)
Hungarian Academy of Sciences
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.EBI
J Med Chem 40: 980-9 (1997)
Boehringer Ingelheim Pharmaceuticals Inc
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI
J Med Chem 40: 952-60 (1997)
Cooperation Pharmaceutique Fran�aise
Depsides and depsidones as inhibitors of HIV-1 integrase: discovery of novel inhibitors through 3D database searching.EBI
J Med Chem 40: 942-51 (1997)
National Cancer Institute-Bethesda
Hydrazide-containing inhibitors of HIV-1 integrase.EBI
J Med Chem 40: 937-41 (1997)
National Cancer Institute-Bethesda
Discovery of HIV-1 integrase inhibitors by pharmacophore searching.EBI
J Med Chem 40: 930-6 (1997)
National Cancer Institute-Bethesda
HIV-1 integrase pharmacophore: discovery of inhibitors through three-dimensional database searching.EBI
J Med Chem 40: 920-9 (1997)
National Cancer Institute-Bethesda
Design, synthesis, and biological activities of four angiotensin II receptor ligands with gamma-turn mimetics replacing amino acid residues 3-5.EBI
J Med Chem 40: 903-19 (1997)
Uppsala University
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.BDB
J Med Chem 40: 885-97 (1997)
Uppsala University
Synthesis and pharmacology of novel analogues of oxytocin and deaminooxytocin: directed methods for the construction of disulfide and trisulfide bridges in peptides.EBI
J Med Chem 40: 864-76 (1997)
University of Minnesota
Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives.EBI
J Med Chem 40: 858-63 (1997)
University of New Orleans
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.EBI
J Med Chem 40: 851-7 (1997)
National Institutes of Health
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.EBI
J Med Chem 40: 841-50 (1997)
Glaxo Wellcome S.p.A.
GRID/GOLPE 3D quantitative structure-activity relationship study on a set of benzamides and naphthamides, with affinity for the dopamine D3 receptor subtype.EBI
J Med Chem 40: 833-40 (1997)
University Centre for Pharmacy
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.EBI
J Med Chem 40: 830-2 (1997)
Merck Research Laboratories
Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs.BDB
J Neuropsychiatry Clin Neurosci 8: 223-6 (1996)
TBA
Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR).EBI
J Pharmacol Exp Ther 280: 1304-11 (1997)
Sankyo Co., Ltd
Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.BDB
J Pharmacol Exp Ther 280: 1241-9 (1997)
Institut de Recherches Servier
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.EBI
J Med Chem 40: 819-24 (1997)
Abbott Laboratories
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.EBI
J Med Chem 40: 754-65 (1997)
Merck Sharp and Dohme Research Laboratories
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.EBI
J Med Chem 40: 749-53 (1997)
University of Washington
Three-dimensional quantitative structure-activity relationship of melatonin receptor ligands: a comparative molecular field analysis study.EBI
J Med Chem 40: 739-48 (1997)
Universit£ de Paris-Sud
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.EBI
J Med Chem 40: 730-8 (1997)
CoCensys Inc
From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus.EBI
J Med Chem 40: 717-29 (1997)
Genentech
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.EBI
J Med Chem 40: 705-16 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid rEBI
J Med Chem 40: 695-704 (1997)
National Institute of Diabetes and Digestive and Kidney Diseases
2D 3D