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Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.EBI
J Med Chem 43: 3453-73 (2000)
Cor Therapeutics
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.EBI
Bioorg Med Chem Lett 10: 2141-4 (2000)
University Of Amsterdam
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.EBI
Bioorg Med Chem Lett 10: 2137-40 (2000)
Celltech-Chiroscience
Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.EBI
Bioorg Med Chem Lett 10: 2119-22 (2000)
Neurogen
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.EBI
Bioorg Med Chem Lett 10: 2111-4 (2000)
Merck Research Laboratories
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.EBI
Bioorg Med Chem Lett 10: 2087-90 (2000)
Kyoto University
Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase.EBI
Bioorg Med Chem Lett 10: 2079-81 (2000)
Pharmacia
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.EBI
Bioorg Med Chem Lett 10: 2071-4 (2000)
Institute
Computational binding studies of human pp60c-src SH2 domain with a series of nonpeptide, phosphophenyl-containing ligands.EBI
Bioorg Med Chem Lett 10: 2067-70 (2000)
Yale University
A novel inhibitor of human telomerase derived from 10H-indolo[3,2-b]quinoline.EBI
Bioorg Med Chem Lett 10: 2063-6 (2000)
Reading University
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.EBI
Bioorg Med Chem Lett 10: 2051-4 (2000)
Bayer Research Center
Discovery of a new class of p38 kinase inhibitors.EBI
Bioorg Med Chem Lett 10: 2047-50 (2000)
Bayer Research Center
Specificity and mechanism of action of some commonly used protein kinase inhibitors.EBI
Biochem J 351: 95-105 (2001)
University Of Dundee
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.BDB
Eur J Biochem 267: 5983-94 (2000)
Cnrs
Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in gene transfectant systems.EBI
Drug Metab Dispos 28: 1238-43 (2000)
University Of Tokyo
Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors.BDB
J Pharmacol Exp Ther 295: 337-45 (2000)
Cocensys
Cannabinoid agonist signal transduction in rat brain: comparison of cannabinoid agonists in receptor binding, G-protein activation, and adenylyl cyclase inhibition.BDB
J Pharmacol Exp Ther 295: 328-36 (2000)
Wake Forest University
Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1.EBI
J Pharmacol Exp Ther 295: 261-5 (2000)
Kyoto University Hospital
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.BDB
J Pharmacol Exp Ther 295: 226-32 (2000)
Albany Medical College
Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.EBI
J Pharmacol Exp Ther 295: 10-5 (2000)
Gilead Sciences
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.EBI
Bioorg Med Chem Lett 10: 2041-4 (2001)
Friedrich-Alexander University
Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1.EBI
Bioorg Med Chem Lett 10: 2037-9 (2001)
Novartis Institute For Biomedical Research
Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation.EBI
Bioorg Med Chem Lett 10: 2023-6 (2001)
Université
Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids.EBI
Bioorg Med Chem Lett 10: 1995-9 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.EBI
Bioorg Med Chem Lett 10: 1991-4 (2001)
Wyeth-Ayerst Research
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.EBI
Bioorg Med Chem Lett 10: 1975-8 (2001)
Merck Research Laboratories
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.EBI
Bioorg Med Chem Lett 10: 1971-3 (2001)
Merck Research Laboratories
The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.EBI
Bioorg Med Chem Lett 10: 1949-52 (2001)
Astrazeneca Pharmaceuticals
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.EBI
Bioorg Med Chem Lett 10: 1943-8 (2001)
Merck Research Laboratories
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.EBI
Bioorg Med Chem Lett 10: 1917-20 (2001)
Merck Research Laboratories
Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase.EBI
Bioorg Med Chem Lett 10: 1909-11 (2001)
University Of Canterbury
Human liver glycogen phosphorylase inhibitors bind at a new allosteric site.BDB
Chem Biol 7: 677-82 (2000)
Pfizer
Workup-dependent formation of 5-lipoxygenase inhibitory boswellic acid analogues.EBI
J Nat Prod 63: 1058-61 (2000)
Institute Of Pharmaceutical Sciences
Structure-activity studies including a Psi(CH(2)-NH) scan of peptide YY (PYY) active site, PYY(22-36), for interaction with rat intestinal PYY receptors: development of analogues with potent in vivo activity in the intestine.EBI
J Med Chem 43: 3420-7 (2000)
University Of Cincinnati Medical Center
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.EBI
J Med Chem 43: 3408-19 (2000)
Cocensys
Synthesis and biological activity of a novel 11a-homo (cyclohexyl) prostaglandin.EBI
J Med Chem 43: 3400-7 (2000)
Alcon Laboratories
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.EBI
J Med Chem 43: 3386-99 (2000)
Merck Research Laboratories
Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.EBI
J Med Chem 43: 3372-6 (2000)
Suntory Biomedical Research
Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.EBI
J Med Chem 43: 3351-71 (2000)
Basf Bioresearch
Biochemical and cellular effects of c-Src kinase-selective pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.BDB
Biochem Pharmacol 60: 885-98 (2000)
Parke-Davis Pharmaceutical Research
Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate.EBI
Biochem Biophys Res Commun 275: 831-8 (2000)
Tohoku University School Of Medicine
Arylsulfonyl-N,N-diethyl-dithiocarbamates: a novel class of antitumor agents.EBI
Bioorg Med Chem Lett 10: 1887-91 (2000)
Università
Synthesis and HIV-1 integrase inhibitory activities of caffeoylglucosides.EBI
Bioorg Med Chem Lett 10: 1879-82 (2000)
Institute Of Science And Technology
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.EBI
Bioorg Med Chem Lett 10: 1875-8 (2000)
Shionogi
Aminoalkyl adenylate and aminoacyl sulfamate intermediate analogues differing greatly in affinity for their cognate Staphylococcus aureus aminoacyl tRNA synthetases.EBI
Bioorg Med Chem Lett 10: 1871-4 (2000)
Smithkline Beecham Pharmaceuticals
1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.EBI
Bioorg Med Chem Lett 10: 1867-70 (2000)
Smithkline Beecham Pharmaceuticals
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.EBI
Bioorg Med Chem Lett 10: 1863-6 (2000)
Smithkline Beecham Pharmaceuticals
A solid-phase synthesis for beta-turn mimetics of sialyl Lewis X.EBI
Bioorg Med Chem Lett 10: 1827-30 (2000)
Nippon Organon K.K.
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.BDB
Bioorg Med Chem Lett 10: 1819-22 (2000)
Korea Research Institute Of Bioscience And Biotechnology
Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of four stereoisomeric analogues of the natural product SB-219383.EBI
Bioorg Med Chem Lett 10: 1811-4 (2000)
Smithkline Beecham Pharmaceuticals
4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.EBI
Bioorg Med Chem Lett 10: 1807-10 (2000)
Eli Lilly
CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.EBI
Bioorg Med Chem Lett 10: 1803-6 (2000)
Smithkline Beecham Pharmaceuticals
Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(2''-, 3''- or 4''-substituted) biphenyltropanes.EBI
Bioorg Med Chem Lett 10: 1783-5 (2000)
Yale University
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.EBI
Am J Physiol Renal Physiol 279: 449-58 (2000)
Medical College Of Georgia
3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.EBI
J Med Chem 43: 3348-50 (2000)
University Of Bristol
Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand.EBI
J Med Chem 43: 3344-7 (2000)
The University Of Michigan Medical School
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.EBI
J Med Chem 43: 3335-43 (2000)
Freie UniversitäT Berlin
Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.EBI
J Med Chem 43: 3283-94 (2000)
Georgetown University Medical Center
4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.BDB
J Med Chem 43: 3244-56 (2000)
Wyeth-Ayerst Research
GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.EBI
J Med Chem 43: 3233-43 (2000)
University Of Perugia
Crystal structures of human factor Xa complexed with potent inhibitors.BDB
J Med Chem 43: 3226-32 (2000)
Aventis Pharma
Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.EBI
J Med Chem 43: 3209-17 (2000)
National Cancer Institute-Bethesda
Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.BDB
J Mol Biol 302: 155-70 (2000)
Cnrs
The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor.BDB
Neuropharmacology 39: 2044-53 (2000)
University Of Frankfurt
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.EBI
J Med Chem 43: 3193-6 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents.EBI
J Med Chem 43: 3168-85 (2000)
Pfizer
Use of an additional hydrophobic binding site, the Z site, in the rational drug design of a new class of stronger trypanothione reductase inhibitor, quaternary alkylammonium phenothiazines.EBI
J Med Chem 43: 3148-56 (2000)
University Of Manchester
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).BDB
J Med Chem 43: 3134-47 (2000)
University Of Auckland
Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.EBI
J Med Chem 43: 3125-33 (2000)
Duquesne University
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.EBI
J Med Chem 43: 3118-24 (2000)
Universita' Di Firenze
Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.EBI
J Med Chem 43: 3111-7 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines.EBI
J Med Chem 43: 3103-10 (2000)
Centre For Addiction And Mental Health
1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists.EBI
J Med Chem 43: 3074-84 (2000)
Virginia Commonwealth University
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.EBI
J Med Chem 43: 3045-51 (2000)
Georgetown University Medical Center
GRID/CPCA: a new computational tool to design selective ligands.EBI
J Med Chem 43: 3033-44 (2000)
Boehringer Ingelheim Pharma
DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors.EBI
J Med Chem 43: 3020-32 (2000)
Eli Lilly
CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors.EBI
J Med Chem 43: 3005-19 (2000)
University Of Texas
Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.EBI
J Med Chem 43: 2992-3004 (2000)
University Of Catania
2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.EBI
J Med Chem 43: 2982-91 (2000)
Organix
Identification of a chemical tool for the orphan nuclear receptor FXR.EBI
J Med Chem 43: 2971-4 (2000)
Glaxo Wellcome Research & Development
Synthesis and evaluation of peptidomimetics as selective inhibitors and active site probes of nitric oxide synthases.EBI
J Med Chem 43: 2938-45 (2000)
Northwestern University
Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl(omega-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate iodide, calcium channel antagonists.EBI
J Med Chem 43: 2906-14 (2000)
State University Of New York
Adenosine kinase inhibitors. 2. Synthesis, enzyme inhibition, and antiseizure activity of diaryltubercidin analogues.EBI
J Med Chem 43: 2894-905 (2000)
Metabasis Therapeutics
Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues.EBI
J Med Chem 43: 2883-93 (2000)
Metabasis Therapeutics
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).EBI
J Med Chem 43: 2871-82 (2000)
University Centre For Pharmacy
Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.EBI
J Med Chem 43: 2860-70 (2000)
Vanderbilt University School Of Medicine
Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor.EBI
J Med Chem 43: 2837-50 (2000)
Astrazeneca R&D SöDertäLje
Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.EBI
J Med Chem 43: 2831-6 (2000)
Institute Of Science
Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.EBI
J Med Chem 43: 2824-30 (2000)
Institute Of Science
A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.EBI
J Med Chem 43: 2814-23 (2000)
Universit£
Further studies on nociceptin-related peptides: discovery of a new chemical template with antagonist activity on the nociceptin receptor.EBI
J Med Chem 43: 2805-13 (2000)
University Of Ferrara
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.BDB
J Med Chem 43: 2797-804 (2000)
University Of Newcastle
A refined 3-dimensional QSAR of cytochrome P450 2C9: computational predictions of drug interactions.EBI
J Med Chem 43: 2789-96 (2000)
Washington State University
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.EBI
J Med Chem 43: 2775-8 (2000)
Synaptic Pharmaceutical
Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.BDB
J Pharmacol Exp Ther 294: 1154-65 (2000)
Smithkline Beecham Pharmaceuticals
The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats.BDB
J Biol Chem 275: 36043-8 (2000)
Federal Institute Of Technology Of Zurich
Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.EBI
Bioorg Med Chem Lett 10: 1771-3 (2000)
Queen'S University Belfast
Grignard-mediated synthesis and preliminary biological evaluation of novel 3-substituted farnesyl diphosphate analogues.EBI
Bioorg Med Chem Lett 10: 1763-6 (2000)
Wayne State University
Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 10: 1745-8 (2000)
University Of Barcelona
Nonbenzamidine compounds as selective factor Xa inhibitors.EBI
Bioorg Med Chem Lett 10: 1737-9 (2000)
Aventis Pharmaceuticals
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.BDB
Bioorg Med Chem Lett 10: 1729-31 (2000)
Dupont Pharmaceuticals
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.EBI
Bioorg Med Chem Lett 10: 1723-7 (2000)
Merck Research Laboratories
6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.EBI
Bioorg Med Chem Lett 10: 1719-21 (2000)
Nps Allelix
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.EBI
Bioorg Med Chem Lett 10: 1707-9 (2000)
Nps Allelix
Anhydride modified cantharidin analogues: synthesis, inhibition of protein phosphatases 1 and 2A and anticancer activity.EBI
Bioorg Med Chem Lett 10: 1687-90 (2000)
The University Of Newcastle
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.EBI
Bioorg Med Chem Lett 10: 1681-6 (2000)
Georgetown University Medical Center
Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.EBI
Bioorg Med Chem Lett 10: 1669-71 (2000)
University Of Tokyo
Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.EBI
Bioorg Med Chem Lett 10: 1665-8 (2000)
Sankyo
Novel inhibitors of AP-1 and NF-kappaB mediated gene expression: structure-activity relationship studies of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)++ +pyrimidi ne-5-carboxylate.EBI
Bioorg Med Chem Lett 10: 1645-8 (2000)
Signal Pharmaceuticals
N-acylated alpha-(3-pyridylmethyl)-beta-aminotetralin antagoinists of the human neuropeptide Y Y5 receptor.EBI
Bioorg Med Chem Lett 10: 1641-3 (2000)
The R. W. Johnson Pharmaceutical Research Institute
Solid-phase synthesis of an arylsulfone hydroxamate library.EBI
Bioorg Med Chem Lett 10: 1637-40 (2000)
Rhone-Poulenc Rorer
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.EBI
Bioorg Med Chem Lett 10: 1625-8 (2000)
Merck
Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.EBI
Bioorg Med Chem Lett 10: 1621-4 (2000)
Merck
Insect nicotinic acetylcholine receptor: conserved neonicotinoid specificity of [(3)H]imidacloprid binding site.EBI
J Neurochem 75: 1294-303 (2000)
University Of California
Fluorescence-based assay for the interaction of small molecules with the human renal organic anion transporter 1.EBI
Anal Biochem 283: 49-55 (2000)
Gilead Sciences
Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.BDB
J Mol Biol 301: 465-75 (2000)
Max-Planck-Institut Fuer Biochemie
Michael adducts of ascorbic acid as inhibitors of protein phosphatase 2A and inducers of apoptosis.EBI
Bioorg Med Chem Lett 10: 1605-8 (2000)
UniversitäT GöTtingen
Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.EBI
Bioorg Med Chem Lett 10: 1597-600 (2000)
University Of Regensburg
Difluoroketones as inhibitors of matrix metalloprotease-13.EBI
Bioorg Med Chem Lett 10: 1581-4 (2000)
Pfizer
Kinetic characterisation of ene-diol-based inhibitors of alpha-amylase.EBI
Bioorg Med Chem Lett 10: 1575-6 (2000)
University Of Canterbury
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.EBI
Bioorg Med Chem Lett 10: 1567-70 (2000)
Novartis Horsham Research Centre
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.EBI
Bioorg Med Chem Lett 10: 1563-6 (2000)
Novartis Horsham Research Centre
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.EBI
Bioorg Med Chem Lett 10: 1559-62 (2000)
Inha University
1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors.EBI
Bioorg Med Chem Lett 10: 1555-8 (2000)
Novartis Institute For Biomedical Research
Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes.EBI
Bioorg Med Chem Lett 10: 1535-8 (2000)
Wyeth-Ayerst Research
Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.EBI
Bioorg Med Chem Lett 10: 1531-4 (2000)
Merck Research Laboratories
Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.EBI
Bioorg Med Chem Lett 10: 1527-30 (2000)
Merck Research Laboratories
Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase.EBI
Bioorg Med Chem Lett 10: 1523-6 (2000)
The University Of Montana
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.EBI
Bioorg Med Chem Lett 10: 1519-22 (2000)
Procter & Gamble Pharmaceuticals
Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors.EBI
Bioorg Med Chem Lett 10: 1497-9 (2000)
Millennium Pharmaceutical
Recognition of a cognate RNA aptamer by neomycin B: quantitative evaluation of hydrogen bonding and electrostatic interactions.BDB
Nucleic Acids Res 28: 2935-42 (2000)
The Ohio State University
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.BDB
Chem Biol 7: 493-504 (2000)
Novartis Pharmaceuticals
Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.EBI
Drug Metab Dispos 28: 895-8 (2000)
Vanderbilt University School Of Medicine
Agonist-directed trafficking of porcine alpha(2A)-adrenergic receptor signaling in Chinese hamster ovary cells: l-isoproterenol selectively activates G(s).BDB
J Pharmacol Exp Ther 294: 539-47 (2000)
University Of Michigan
A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.EBI
J Med Chem 43: 2770-4 (2000)
Combichem
Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.EBI
J Med Chem 43: 2759-69 (2000)
University Of Minnesota
Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.EBI
J Med Chem 43: 2738-44 (2000)
National Center For Genetic Engineering And Biotechnology At Thailand
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.EBI
J Med Chem 43: 2731-7 (2000)
Arizona State University
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.EBI
J Med Chem 43: 2703-18 (2000)
Merck Research Laboratories
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.EBI
J Med Chem 43: 2698-702 (2000)
University Of California
Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.EBI
J Med Chem 43: 2685-97 (2000)
Université
Synthesis and antitumor activity of new benzoheterocyclic derivatives of distamycin A.EBI
J Med Chem 43: 2675-84 (2000)
Universit£
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.BDB
J Med Chem 43: 2655-63 (2000)
Sugen
Ligands for glutamate receptors: design and therapeutic prospects.EBI
J Med Chem 43: 2609-45 (2000)
The Royal Danish School Of Pharmacy
Novel nonsubstrate inhibitors of human thymidine phosphorylase, a potential target for tumor-dependent angiogenesis.EBI
J Med Chem 43: 2601-7 (2000)
Istituto Di Genetica Biochimica Ed Evoluzionistica
Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.EBI
J Med Chem 43: 2586-90 (2000)
University Of Northern Colorado
Aureobasidins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC-transporter.EBI
J Med Chem 43: 2547-56 (2000)
Strasbourg 1 University
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.EBI
J Med Chem 43: 2523-9 (2000)
Eisai
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.EBI
J Med Chem 43: 2514-22 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.BDB
J Med Chem 43: 2506-13 (2000)
Palacky University
Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.EBI
J Med Chem 43: 2489-92 (2000)
University Of Minnesota
Structure-based design and solid-phase parallel synthesis of phosphorylated nonpeptides to explore hydrophobic binding at the Src SH2 domain.BDB
J Comb Chem 2: 305-13 (2000)
Ariad Pharmaceuticals
Synthesis and biological activities of an alpha-methyl and a beta-methyl carbapenem and the corresponding unsubstituted compound.EBI
Bioorg Med Chem Lett 10: 1389-91 (2000)
University Of Munich
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.EBI
Bioorg Med Chem Lett 10: 1381-4 (2000)
Merck Sharp & Dohme Research Laboratories
Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 10: 1377-80 (2000)
Zentrum FüR Pharmaforschung
Convergent synthesis of ribonuclease L-active 2',5'-oligoadenylate-peptide nucleic acids.EBI
Bioorg Med Chem Lett 10: 1357-60 (2000)
National Institute Of Diabetes And Digestive Antd Kidney Diseases
Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.EBI
Bioorg Med Chem Lett 10: 1351-5 (2000)
Hoechst Marion Roussel
Synthesis and uptake of nitric oxide-releasing drugs by the P2 nucleoside transporter in Trypanosoma equiperdum.EBI
Bioorg Med Chem Lett 10: 1347-50 (2000)
Universit£
Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.EBI
Bioorg Med Chem Lett 10: 1315-6 (2000)
Kitasato University
Synthesis of N-diisopropyl phosphoryl benzyltetrahydroisoquinoline, a new class of mitochondrial complexes I and III inhibitors.EBI
Bioorg Med Chem Lett 10: 1491-4 (2000)
Universidad De Valencia
Potent new leucine aminopeptidase inhibitor of novel structure synthesised by a modified Wadsworth-Emmons (Horner) Wittig procedure.EBI
Bioorg Med Chem Lett 10: 1481-2 (2000)
The Queen'S University Of Belfast
Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.EBI
Bioorg Med Chem Lett 10: 1471-5 (2000)
The Scripps Research Institute
N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: an orally active neurokinin NK1/NK2 antagonist.EBI
Bioorg Med Chem Lett 10: 1467-70 (2000)
Novartis Pharma
Synthesis and structure-activity relationships of novel fungal chitin synthase inhibitors.EBI
Bioorg Med Chem Lett 10: 1459-62 (2000)
Nippon Roche Research Center
Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers.EBI
Bioorg Med Chem Lett 10: 1455-7 (2000)
Korea Research Institute Of Bioscience And Biotechnology
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.EBI
Bioorg Med Chem Lett 10: 1447-50 (2000)
Università
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.EBI
Bioorg Med Chem Lett 10: 1443-6 (2000)
Georgetown University Medical Center
Synthesis of tetrakis(multifluoro-4-pyridyl)porphin derivatives as acetylcholinesterase inhibitors.EBI
Bioorg Med Chem Lett 10: 1435-8 (2000)
Seoul National University
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.EBI
Bioorg Med Chem Lett 10: 1431-4 (2000)
Merck Research Laboratories
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.EBI
Bioorg Med Chem Lett 10: 1427-9 (2000)
Merck Research Laboratories
Antifungal rapamycin analogues with reduced immunosuppressive activity.EBI
Bioorg Med Chem Lett 10: 1405-8 (2000)
Abbott Laboratories
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.EBI
J Med Chem 43: 2479-83 (2000)
Rational Drug Design Laboratories
6-N-Acyltriciribine analogues: structure-activity relationship between acyl carbon chain length and activity against HIV-1.EBI
J Med Chem 43: 2457-63 (2000)
University Of Michigan
Deoxy sugar analogues of triciribine: correlation of antiviral and antiproliferative activity with intracellular phosphorylation.EBI
J Med Chem 43: 2438-48 (2000)
University Of Michigan
Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.EBI
J Med Chem 43: 2419-29 (2000)
Purdue University
A rational approach to the design and synthesis of a new bradykinin B(1) receptor antagonist.EBI
J Med Chem 43: 2387-94 (2000)
University Of Montpellier
Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.EBI
J Med Chem 43: 2382-6 (2000)
University Of Montpellier
Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.EBI
J Med Chem 43: 2362-70 (2000)
The James Black Foundation
Synthesis and biological evaluation of bombesin constrained analogues.EBI
J Med Chem 43: 2356-61 (2000)
University Of Montpellier
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.EBI
J Med Chem 43: 2350-5 (2000)
Astrazeneca R&D Boston
17beta-O-Aminoalkyloximes of 5beta-androstane-3beta,14beta-diol with digitalis-like activity: synthesis, cardiotonic activity, structure-activity relationships, and molecular modeling of the Na(+),K(+)-ATPase receptor.EBI
J Med Chem 43: 2332-49 (2000)
Prassis Istituto Di Ricerche Sigma-Tau
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.EBI
J Med Chem 43: 2324-31 (2000)
F. Hoffmann-La Roche
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.BDB
J Med Chem 43: 2310-23 (2000)
Novartis Pharmaceuticals
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.EBI
J Med Chem 43: 2300-9 (2000)
Universit£
Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease.EBI
J Med Chem 43: 2297-9 (2000)
Amgen
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.EBI
J Med Chem 43: 2293-6 (2000)
Pfizer
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.BDB
Bioorg Med Chem 8: 957-75 (2000)
Alcon Research
Cyclobutane carboxamide inhibitors of fungal melanin: biosynthesis and their evaluation as fungicides.EBI
Bioorg Med Chem 8: 897-907 (2000)
Stine Haskell Research Center
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.BDB
J Pharmacol Exp Ther 293: 1048-62 (2000)
Centre De Recherches De Croissy
Trans-stimulation effects of folic acid derivatives on methotrexate transport by rat renal organic anion transporter, OAT-K1.EBI
J Pharmacol Exp Ther 293: 1034-9 (2000)
Kyoto University Hospital
Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.BDB
J Pharmacol Exp Ther 293: 771-8 (2000)
R. W. Johnson Pharmaceutical Research Institute
Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2.EBI
Hepatology 32: 82-6 (2000)
University Of Zurich
The application of HPLC with on-line coupled UV/MS-biochemical detection for isolation of an acetylcholinesterase inhibitor from narcissus 'Sir Winston Churchill'.EBI
J Nat Prod 63: 803-6 (2000)
Leiden University
Antifungal substances against pathogenic fungi, talaroconvolutins, from talaromyces convolutus.EBI
J Nat Prod 63: 768-72 (2000)
Hoshi University
Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla.EBI
J Nat Prod 63: 753-6 (2000)
Seoul National University
Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases.EBI
J Nat Prod 63: 739-45 (2000)
Heinrich-Heine-UniversitäT
Thermodynamics of sequence-specific binding of PNA to DNA.BDB
Biochemistry 39: 7781-91 (2000)
Chalmers University Of Technology
Discovery of a potent, non-triketone type inhibitor of 4-hydroxyphenylpyruvate dioxygenase.EBI
Bioorg Med Chem Lett 10: 1297-8 (2000)
Tunghai Christian University
Total synthesis of pyrrolizidines 223H', 239K', 265H', and 267H' found in Madagascan frogs (Mantella) and their affinities for nicotinic acetylcholine receptor.EBI
Bioorg Med Chem Lett 10: 1293-5 (2000)
Toyama Medical And Pharmaceutical University
4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.EBI
Bioorg Med Chem Lett 10: 1281-4 (2000)
Research Triangle Institute
Conformationally-restricted ligands for the histamine H1 receptor.EBI
Bioorg Med Chem Lett 10: 1277-9 (2000)
University Of Bath
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.EBI
Bioorg Med Chem Lett 10: 1261-4 (2000)
Novartis Pharma
Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.BDB
Bioorg Med Chem Lett 10: 1257-60 (2000)
Gilead Sciences
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.EBI
Bioorg Med Chem Lett 10: 1253-6 (2000)
Dupont Pharmaceuticals
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.EBI
Bioorg Med Chem Lett 10: 1245-8 (2000)
Ccipe-Faculte De Pharmacie
(+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist.EBI
Bioorg Med Chem Lett 10: 1241-4 (2000)
Novartis Pharma
'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker.EBI
Bioorg Med Chem Lett 10: 1227-31 (2000)
Kyoto Pharmaceutical University
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.EBI
Bioorg Med Chem Lett 10: 1219-21 (2000)
The Oxford Centre For Molecular Sciences
Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.EBI
Bioorg Med Chem Lett 10: 1185-8 (2000)
Universit£
Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.EBI
Bioorg Med Chem Lett 10: 1175-9 (2000)
Novartis Pharma
The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic.EBI
Bioorg Med Chem Lett 10: 1171-3 (2000)
Roche Research Center
Cyclic thioether peptide mimetics as VCAM-VLA-4 antagonists.EBI
Bioorg Med Chem Lett 10: 1167-9 (2000)
Roche Research Center
Carbacyclic peptide mimetics as VCAM-VLA-4 antagonists.EBI
Bioorg Med Chem Lett 10: 1163-5 (2000)
Roche Research Center
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.BDB
Bioorg Med Chem Lett 10: 1159-62 (2000)
Glaxosmithkline
Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1.EBI
Eur J Pharmacol 398: 193-7 (2000)
Kyoto University Hospital
Behaviroal, pharmacological, and molecular characterization of an amphibian cannabinoid receptor.BDB
J Neurochem 75: 413-23 (2000)
Oregon State University
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.EBI
Bioorg Med Chem Lett 10: 997-9 (2000)
Celltech Chiroscience
Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.EBI
Bioorg Med Chem Lett 10: 993-5 (2000)
Celltech Chiroscience
Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.EBI
Bioorg Med Chem Lett 10: 983-7 (2000)
Corvas International
Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2.EBI
Bioorg Med Chem Lett 10: 979-81 (2000)
University Of Wales
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI
Bioorg Med Chem Lett 10: 963-6 (2000)
Berlex Biosciences
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.EBI
Bioorg Med Chem Lett 10: 957-61 (2000)
Berlex Biosciences
Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.EBI
Bioorg Med Chem Lett 10: 945-9 (2000)
Novartis Pharma
Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.EBI
Bioorg Med Chem Lett 10: 923-7 (2000)
National Cancer Institute-Bethesda
Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.EBI
Bioorg Med Chem Lett 10: 919-21 (2000)
Nps Allelix
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.EBI
Bioorg Med Chem Lett 10: 903-5 (2000)
Nps Allelix
Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.EBI
Bioorg Med Chem Lett 10: 895-7 (2000)
Iowa State University
Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity.EBI
Bioorg Med Chem Lett 10: 875-9 (2000)
Yoshitomi Pharmaceutical Industries
Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists.EBI
Bioorg Med Chem Lett 10: 859-63 (2000)
Kyoto University
The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.EBI
Bioorg Med Chem Lett 10: 853-7 (2000)
Southern Methodist University
The synthesis and evaluation of 2-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.EBI
Bioorg Med Chem Lett 10: 847-51 (2000)
Southern Methodist University
SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.EBI
Bioorg Med Chem Lett 10: 843-5 (2000)
Tunghai Christian University
Characterization of the human cysteinyl leukotriene 2 receptor.BDB
J Biol Chem 275: 30531-6 (2000)
University Of Virginia
Polyoxygenated dysidea sterols that inhibit the binding of [I125] IL-8 to the human recombinant IL-8 receptor type A.EBI
J Nat Prod 63: 694-7 (2000)
Griffith University
Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV.EBI
Bioorg Med Chem Lett 10: 1117-20 (2000)
Universit£
Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.EBI
Bioorg Med Chem Lett 10: 1113-5 (2000)
Yale University
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.EBI
Bioorg Med Chem Lett 10: 1109-11 (2000)
R. W. Johnson Pharmaceutical Research Institute
First pharmacophoric hypothesis for 5-HT7 antagonism.EBI
Bioorg Med Chem Lett 10: 1097-100 (2000)
Universidad Complutense
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.EBI
Bioorg Med Chem Lett 10: 1093-6 (2000)
The R. W. Johnson Pharmaceutical Research Institute
High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor.EBI
Bioorg Med Chem Lett 10: 1089-92 (2000)
Università
Novel alpha-glucosidase inhibitors with a tetrachlorophthalimide skeleton.EBI
Bioorg Med Chem Lett 10: 1081-4 (2000)
University Of Tokyo
Examination of N-hydroxylation as a prerequisite mechanism of nitric oxide synthase inactivation.EBI
Bioorg Med Chem Lett 10: 1077-80 (2000)
University At Buffalo
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.EBI
Bioorg Med Chem Lett 10: 1069-72 (2000)
Merck Research Laboratories
Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor.EBI
Bioorg Med Chem Lett 10: 1063-6 (2000)
R. W. Johnson Pharmaceutical Research Institute
Structure-activity relationship studies of flavopiridol analogues.EBI
Bioorg Med Chem Lett 10: 1037-41 (2000)
Mitotix
Synthesis of glycolipid analogues that disrupt binding of HIV-1 gp120 to galactosylceramide.EBI
Bioorg Med Chem Lett 10: 1011-4 (2000)
Cornell University
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.EBI
Bioorg Med Chem Lett 10: 1007-10 (2000)
Glaxo Wellcome
Modeling cyclooxygenase inhibition. Implication of active site hydration on the selectivity of ketoprofen analogues.EBI
J Med Chem 43: 2280-4 (2000)
Laboratorios Menarini
Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.EBI
J Med Chem 43: 2248-57 (2000)
Novartis Institute For Biomedical Research
Novel inhibitors of nucleoside triphosphate diphosphohydrolases: chemical synthesis and biochemical and pharmacological characterizations.EBI
J Med Chem 43: 2239-47 (2000)
Universit£
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.EBI
J Med Chem 43: 2227-38 (2000)
Vrije Universiteit
Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.EBI
J Med Chem 43: 2217-26 (2000)
Neurosearch
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.EBI
J Med Chem 43: 2196-203 (2000)
National Institute Of Diabetes
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI
J Med Chem 43: 2183-95 (2000)
The R. W. Johnson Pharmaceutical Research Institute
Structure-activity relationships in a series of bisquaternary bisphthalimidine derivatives modulating the muscarinic M(2)-receptor allosterically.EBI
J Med Chem 43: 2155-64 (2000)
University Of W�Rzburg
Modeling of kappa-opioid receptor/agonists interactions using pharmacophore-based and docking simulations.EBI
J Med Chem 43: 2124-34 (2000)
Universit£
Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.EBI
J Med Chem 43: 2115-23 (2000)
Istituto Di Chimica Farmaceutica E Tossicologica
Developing a dynamic pharmacophore model for HIV-1 integrase.EBI
J Med Chem 43: 2100-14 (2000)
University Of California
Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs.EBI
Proc Natl Acad Sci U S A 97: 7476-81 (2000)
The Netherlands Cancer Institute
[3H]S33084: a novel, selective and potent radioligand at cloned, human dopamine D3 receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 361: 569-72 (2000)
Croissy-Sur-Seine Paris
Role of organic cation transporters in the renal secretion of nucleosides.EBI
Biochem Pharmacol 60: 215-9 (2000)
The University Of Texas M.D. Anderson Cancer Center
Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta.EBI
Biochim Biophys Acta 1466: 315-27 (2000)
Medical College Of Georgia
Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors.BDB
Br J Pharmacol 130: 692-8 (2000)
Friedrich-Schiller-University Jena
7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.EBI
J Med Chem 43: 2079-81 (2000)
University Of Bonn
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.EBI
J Med Chem 43: 2064-71 (2000)
Georgetown University Medical Center
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety.EBI
J Med Chem 43: 2049-63 (2000)
Takeda Chemical Industries
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.EBI
J Med Chem 43: 2040-8 (2000)
Shionogi
A new class of HIV-1 integrase inhibitors: the 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol family.EBI
J Med Chem 43: 2031-9 (2000)
University Of California
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.BDB
J Med Chem 43: 2019-30 (2000)
Dupont Pharmaceuticals
SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues.BDB
J Med Chem 43: 2007-18 (2000)
University Of Bologna
Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.EBI
J Med Chem 43: 1993-2006 (2000)
Neogenesis
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.EBI
J Med Chem 43: 1958-68 (2000)
Eli Lilly
Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives.EBI
J Med Chem 43: 1949-57 (2000)
Cnrs Umr 8532
Synthesis and evaluation of"AZT-HEPT","AZT-pyridinone", and"ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase.EBI
J Med Chem 43: 1927-39 (2000)
Institut Curie
Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).EBI
J Med Chem 43: 1910-26 (2000)
The Institute Of Cancer Research
Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists.EBI
J Med Chem 43: 1901-9 (2000)
Jagiellonian University
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.EBI
Drug Metab Dispos 28: 655-60 (2000)
Vanderbilt University School Of Medicine
Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806.BDB
Neuropharmacology 39: 1443-50 (2000)
University Of Cambridge
Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.EBI
J Med Chem 43: 1892-7 (2000)
Cocensys
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.BDB
J Med Chem 43: 1886-91 (2000)
Sapienza University Of Rome
Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat.EBI
J Med Chem 43: 1878-85 (2000)
Smithkline Beecham Pharmaceuticals
Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties.EBI
J Med Chem 43: 1858-65 (2000)
Università
Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.EBI
J Med Chem 43: 1852-7 (2000)
University Of Bristol
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.BDB
J Med Chem 43: 1841-51 (2000)
Universitat Des Saarlandes
Multivariate data analysis using D-optimal designs, partial least squares, and response surface modeling: A directional approach for the analysis of farnesyltransferase inhibitors.EBI
J Med Chem 43: 1807-16 (2000)
RhôNe-Poulenc Rorer
Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.EBI
J Med Chem 43: 1793-806 (2000)
Universit£
Design of a Gag pentapeptide analogue that binds human cyclophilin A more efficiently than the entire capsid protein: new insights for the development of novel anti-HIV-1 drugs.EBI
J Med Chem 43: 1770-9 (2000)
Departement D'Ingenierie Et D'Etudes Des Proteines
Solution structures in SDS micelles and functional activity at the bullfrog substance P receptor of ranatachykinin peptides.EBI
J Med Chem 43: 1741-53 (2000)
Marshall University School Of Medicine And Huntington Va Medical Center
Design and synthesis of conformationally constrained glucagon analogues.EBI
J Med Chem 43: 1714-22 (2000)
University Of Arizona
New proline mimetics: synthesis of thrombin inhibitors incorporating cyclopentane- and cyclopentenedicarboxylic acid templates in the P2 position. Binding conformation investigated by X-ray crystallography.EBI
J Med Chem 43: 1705-13 (2000)
Link£Ping University
2-amino-2-oxazolines as subtype selective alpha(2) adrenoceptor agonists.EBI
J Med Chem 43: 1699-704 (2000)
Lundbeck Research Usa
Probing the conformation of the sugar transport inhibitor phlorizin by 2D-NMR, molecular dynamics studies, and pharmacophore analysis.EBI
J Med Chem 43: 1692-8 (2000)
Max-Planck-Institut F£R Molekulare Physiologie
Molecular determinants of MAO selectivity in a series of indolylmethylamine derivatives: biological activities, 3D-QSAR/CoMFA analysis, and computational simulation of ligand recognition.EBI
J Med Chem 43: 1684-91 (2000)
Universitat AutòNoma De Barcelona
Substituted benzamide inhibitors of human rhinovirus 3C protease: structure-based design, synthesis, and biological evaluation.EBI
J Med Chem 43: 1670-83 (2000)
Agouron Pharmaceuticals
Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration.EBI
J Med Chem 43: 1664-9 (2000)
Novo Nordisk
N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration.EBI
J Med Chem 43: 1661-3 (2000)
Pfizer
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.EBI
J Med Chem 43: 1641-60 (2000)
Dupont Pharmaceuticals
Halogenated boldine derivatives with enhanced monoamine receptor selectivity.EBI
J Nat Prod 63: 480-4 (2000)
Universidad De Chile
Bioactive compounds from Combretum erythrophyllum.EBI
J Nat Prod 63: 457-60 (2000)
Virginia Polytechnic Institute And State University
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.EBI
Bioorg Med Chem Lett 10: 831-4 (2000)
F. Hoffmann-La Roche
Leukotriene B4 photoaffinity probes: design, synthesis and evaluation of new arylazide-1,3-disubstituted cyclohexanes.EBI
Bioorg Med Chem Lett 10: 811-4 (2000)
Upresa-Cnrs 5074
Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics.EBI
Bioorg Med Chem Lett 10: 805-9 (2000)
Laboratoires Upsa
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.EBI
Bioorg Med Chem Lett 10: 783-6 (2000)
Wyeth-Ayerst Research
Synthesis of a cyanopeptide-analogue with trypsin activating properties.EBI
Bioorg Med Chem Lett 10: 779-81 (2000)
Ernst-Moritz-Arndt-University
QSAR of 1,1'-(1,2-ethylenebisbenzyl)bis(4-substitutedpyridinium) dibromides as choline kinase inhibitors: a different approach for antiproliferative drug design.EBI
Bioorg Med Chem Lett 10: 767-70 (2000)
Granada
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI
Bioorg Med Chem Lett 10: 745-9 (2000)
Corvas International
N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.EBI
Bioorg Med Chem Lett 10: 729-33 (2000)
Hoffmann-La Roche
N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists.EBI
Bioorg Med Chem Lett 10: 725-7 (2000)
Roche Research Center
Alpha-ketoamides, alpha-ketoesters and alpha-diketones as HCV NS3 protease inhibitors.EBI
Bioorg Med Chem Lett 10: 711-3 (2000)
Dupont Pharmaceuticals
Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor.EBI
Bioorg Med Chem Lett 10: 707-10 (2000)
Niddk
The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.EBI
Bioorg Med Chem Lett 10: 695-8 (2000)
Wyeth-Ayerst Research
Isoxazolines and isoxazoles as factor Xa inhibitors.EBI
Bioorg Med Chem Lett 10: 685-9 (2000)
Dupont Pharmaceuticals
Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities.EBI
J Med Chem 43: 1611-9 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).EBI
J Med Chem 43: 1586-603 (2000)
Abbott Laboratories
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.EBI
J Med Chem 43: 1573-6 (2000)
University Of Minnesota
Structural studies on bioactive compounds. 32. Oxidation of tyrphostin protein tyrosine kinase inhibitors with hypervalent iodine reagents.EBI
J Med Chem 43: 1550-62 (2000)
University Of Nottingham
Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture.EBI
J Med Chem 43: 1533-40 (2000)
Université
AMP deaminase inhibitors. 4. Further N3-substituted coformycin aglycon analogues: N3-alkylmalonates as ribose 5'-monophosphate mimetics.EBI
J Med Chem 43: 1519-24 (2000)
Metabasis Therapeutics
AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues.EBI
J Med Chem 43: 1508-18 (2000)
Metabasis Therapeutics
AMP deaminase inhibitors. 2. Initial discovery of a non-nucleotide transition-state inhibitor series.EBI
J Med Chem 43: 1495-507 (2000)
Metabasis Therapeutics
Study on selectin blocker. 8. Lead discovery of a non-sugar antagonist using a 3D-pharmacophore model.EBI
J Med Chem 43: 1476-83 (2000)
Nippon Organon K.K.
A study of the relationship between biological activity and prolyl amide isomer geometry in oxytocin using 5-tert-butylproline to augment the Cys(6)-Pro(7) amide cis-isomer population.EBI
J Med Chem 43: 1448-55 (2000)
Université
GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.EBI
J Med Chem 43: 1427-47 (2000)
University Of Sydney
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.BDB
Chem Biol 7: 299-312 (2000)
Axys Pharmaceutical
[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.BDB
Mol Pharmacol 57: 968-75 (2000)
University Of Ferrara
Thermodynamic consequences of grafting enhanced affinity toward the mutated antigen onto an antibody. The case of anti-lysozyme antibody, HyHEL-10.BDB
J Biol Chem 275: 12813-20 (2000)
Tohoku University
Distinct Ca2+ binding properties of novel C2 domains of plant phospholipase dalpha and beta.BDB
J Biol Chem 275: 19700-6 (2000)
Kansas State University
Characterization of a tropane radioligand, [(3)H]2beta-propanoyl-3beta-(4-tolyl) tropane ([(3)H]PTT), for dopamine transport sites in rat brain.BDB
J Pharmacol Exp Ther 293: 686-96 (2000)
Wake Forest University
Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein.EBI
J Pharmacol Exp Ther 293: 376-82 (2000)
Dr. Margarete Fischer-Bosch-Institute Of Clinical Pharmacology
Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.EBI
Bioorg Med Chem Lett 10: 681-4 (2000)
Università
Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties.EBI
Bioorg Med Chem Lett 10: 673-6 (2000)
Universit£
Inhibition of the ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties.EBI
Bioorg Med Chem Lett 10: 669-72 (2000)
University Of Paris
Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.EBI
Bioorg Med Chem Lett 10: 653-5 (2000)
National Cancer Institute-Bethesda
The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity.EBI
Bioorg Med Chem Lett 10: 649-52 (2000)
Pharmacia & Upjohn
Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.EBI
Bioorg Med Chem Lett 10: 637-9 (2000)
Cnrs
Parallel synthesis of a library of 1,4-naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi.EBI
Bioorg Med Chem Lett 10: 631-5 (2000)
Université
Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.EBI
Bioorg Med Chem Lett 10: 627-30 (2000)
University Of Tennessee
Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.EBI
Bioorg Med Chem Lett 10: 623-5 (2000)
Eisai
Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.EBI
Bioorg Med Chem Lett 10: 619-22 (2000)
Eisai
Synthesis of a novel class of cdc25A inhibitors from vitamin D3.EBI
Bioorg Med Chem Lett 10: 615-7 (2000)
The University Of Tokyo
ATP-dependent para-aminohippurate transport by apical multidrug resistance protein MRP2.EBI
Kidney Int 57: 1636-42 (2000)
Deutsches Krebsforschungszentrum
Two new prenylated 3-benzoxepin derivatives as cyclooxygenase inhibitors from Perilla frutescens var. acuta.EBI
J Nat Prod 63: 403-5 (2000)
Columbia University
Isolation of psammaplin A 11'-sulfate and bisaprasin 11'-sulfate from the marine sponge Aplysinella rhax.EBI
J Nat Prod 63: 393-5 (2000)
Griffith University
Three new triterpenoids from Peganum nigellastrum.EBI
J Nat Prod 63: 390-2 (2000)
Toho University
Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali.EBI
J Nat Prod 63: 318-21 (2000)
Griffith University
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.EBI
J Nat Prod 63: 315-7 (2000)
Leiden University
18F-labeled FECNT: a selective radioligand for PET imaging of brain dopamine transporters.BDB
Nucl Med Biol 27: 1-12 (2000)
Emory University
In vitro pharmacological profile of SK-896, a new human motilin analogue.BDB
Pharmacology 60: 128-35 (2000)
Sanwa Kagaku Kenkyusho
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI
J Med Chem 43: 1423-6 (2001)
The R. W. Johnson Pharmaceutical Research Institute
Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry.EBI
J Med Chem 43: 1413-7 (2000)
The City University Of New York
Phosphinic derivatives as new dual enkephalin-degrading enzyme inhibitors: synthesis, biological properties, and antinociceptive activities.EBI
J Med Chem 43: 1398-408 (2001)
University Of Paris
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.EBI
J Med Chem 43: 1380-97 (2001)
University Of Auckland
Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.EBI
J Med Chem 43: 1359-66 (2001)
Hungarian Academy Of Sciences
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.EBI
J Med Chem 43: 1339-49 (2001)
Uppsala University
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.EBI
J Med Chem 43: 1329-38 (2001)
F. Hoffmann-La Roche
Novel benzofuran and benzothiophene biphenyls as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties.EBI
J Med Chem 43: 1293-310 (2001)
Wyeth-Ayerst Research
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.BDB
J Med Chem 43: 1282-92 (2000)
Institut Curie
Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing.EBI
J Med Chem 43: 1271-81 (2001)
University Of Queensland
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.EBI
J Med Chem 43: 1257-63 (2001)
Bristol-Myers Squibb Pharmaceutical Research Institute
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.EBI
J Med Chem 43: 1251-2 (2001)
University Of Minnesota
Inhibitory effect of novel oral hypoglycemic agent nateglinide (AY4166) on peptide transporters PEPT1 and PEPT2.EBI
Eur J Pharmacol 392: 11-7 (2000)
Kyoto University Hospital
Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study.BDB
J Biol Chem 275: 16139-45 (2000)
Swiss Federal Institute Of Technology
Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.BDB
J Comb Chem 1: 207-15 (1999)
Smithkline Beecham Pharmaceuticals
N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.EBI
Bioorg Med Chem Lett 10: 509-12 (2000)
Yoshitomi Pharmaceutical Industries
Solid phase synthesis of diamides as potential bone resorption inhibitors.EBI
Bioorg Med Chem Lett 10: 503-7 (2000)
Astrazeneca R & D M£Lndal
Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties.EBI
Bioorg Med Chem Lett 10: 499-502 (2000)
Università
Selection of a potent inhibitor of trihydroxynaphthalene reductase by sorting disease control data.EBI
Bioorg Med Chem Lett 10: 491-4 (2000)
Dupont Pharmaceuticals
The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.EBI
Bioorg Med Chem Lett 10: 483-6 (2000)
State University Of New York
The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: hydroxynaphthalene derivatives.EBI
Bioorg Med Chem Lett 10: 477-81 (2000)
State University Of New York
Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.EBI
Bioorg Med Chem Lett 10: 473-6 (2000)
Albany Molecular Research
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.EBI
Bioorg Med Chem Lett 10: 465-8 (2000)
Università
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.EBI
Bioorg Med Chem Lett 10: 461-4 (2000)
Ewha Womans University
Synthesis and characterization of a novel class of protein tyrosine phosphatase inhibitors.EBI
Bioorg Med Chem Lett 10: 457-60 (2000)
New York University
Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities.EBI
Bioorg Med Chem Lett 10: 453-5 (2000)
Medical University Of South Carolina
Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.EBI
Bioorg Med Chem Lett 10: 449-52 (2000)
Dupont Pharmaceuticals
Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.EBI
Bioorg Med Chem Lett 10: 443-7 (2000)
Merck Research Laboratories
Design and synthesis of mimics of S-adenosyl-L-homocysteine as potential inhibitors of erythromycin methyltransferases.EBI
Bioorg Med Chem Lett 10: 433-7 (2000)
Université
Synthesis and biological activities of NB-506 analogues modified at the glucose group.EBI
Bioorg Med Chem Lett 10: 419-22 (2000)
Banyu Tsukuba Research Institute
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.EBI
Bioorg Med Chem Lett 10: 415-8 (2000)
Ligand Pharmaceuticals
Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.EBI
Bioorg Med Chem Lett 10: 411-4 (2000)
Ligand Pharmaceuticals
Irreversible inhibition of type I dehydroquinase by substrates for type II dehydroquinase.EBI
Bioorg Med Chem Lett 10: 407-9 (2000)
University Chemical Laboratory
Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.EBI
Bioorg Med Chem Lett 10: 605-7 (2000)
University Of Bristol
1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2.EBI
Bioorg Med Chem Lett 10: 601-4 (2000)
The R. W. Johnson Pharmaceutical Research Institute
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.EBI
Bioorg Med Chem Lett 10: 597-600 (2000)
Glaxo Wellcome Research And Development
Naphthyl ketones: a new class of Janus kinase 3 inhibitors.EBI
Bioorg Med Chem Lett 10: 575-9 (2000)
Astrazeneca
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.EBI
Bioorg Med Chem Lett 10: 567-9 (2000)
UniversitäT Hamburg
Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.EBI
Bioorg Med Chem Lett 10: 559-62 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
Parallel synthesis of a series of subtype-selective NMDA receptor antagonists.EBI
Bioorg Med Chem Lett 10: 527-9 (2000)
Parke-Davis Pharmaceutical Research
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.EBI
Bioorg Med Chem Lett 10: 523-6 (2000)
Pfizer
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.EBI
J Med Chem 43: 1234-41 (2000)
Merck Research Laboratories
Novel and selective calcitonin-inducing agents.EBI
J Med Chem 43: 1223-33 (2000)
Wyeth-Ayerst Research
Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors.EBI
J Med Chem 43: 1215-22 (2000)
Georgetown University Medical Center
SH2-directed ligands of the Lck tyrosine kinase.EBI
J Med Chem 43: 1173-9 (2000)
The Albert Einstein College Of Medicine
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.EBI
J Med Chem 43: 1165-72 (2000)
National Institute Of Diabetes
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.EBI
J Med Chem 43: 1158-64 (2000)
Universita' Di Firenze
5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.EBI
J Med Chem 43: 1149-57 (2000)
Merck
Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.EBI
J Med Chem 43: 1135-42 (2000)
Ariad Gene Therapeutics
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.EBI
J Med Chem 43: 1123-34 (2000)
Smithkline Beecham Pharmaceuticals
3D-QSAR CoMFA study on imidazolinergic I(2) ligands: a significant model through a combined exploration of structural diversity and methodology.EBI
J Med Chem 43: 1109-22 (2000)
Universit£
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.BDB
J Med Chem 43: 1094-108 (2000)
Boehringer Ingelheim Pharmaceuticals
Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis.EBI
J Med Chem 43: 1085-93 (2000)
National Institute On Drug Abuse-Intramural Research Program
Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.EBI
J Med Chem 43: 1062-70 (2000)
National Eye Institute
Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.EBI
J Med Chem 43: 1050-61 (2000)
King'S College London
Pyrrolidine inhibitors of human cytosolic phospholipase A(2).EBI
J Med Chem 43: 1041-4 (2000)
Shionogi
Protease inhibitors. Part 8: synthesis of potent Clostridium histolyticum collagenase inhibitors incorporating sulfonylated L-alanine hydroxamate moieties.BDB
Bioorg Med Chem 8: 637-45 (2000)
Universita Degli Studi Di Firenze
Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives.BDB
Bioorg Med Chem 8: 497-506 (2000)
University Of Bologna
Inhibition of the P-glycoprotein- and multidrug resistance protein-mediated efflux of anthracyclines and calceinacetoxymethyl ester by PAK-104P.EBI
Eur J Pharmacol 391: 207-16 (2000)
Universit£
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.BDB
J Med Chem 43: 1034-40 (2000)
Upjohn
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.EBI
J Med Chem 43: 1011-8 (2000)
Virginia Commonwealth University
New azolidinediones as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties.EBI
J Med Chem 43: 995-1010 (2000)
Wyeth-Ayerst Research
Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.EBI
J Med Chem 43: 984-94 (2000)
Cocensys
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.EBI
J Med Chem 43: 945-52 (2000)
Procter And Gamble Pharmaceuticals
Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?EBI
J Med Chem 43: 921-44 (2000)
National Cancer Institute-Bethesda
Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic.EBI
J Med Chem 43: 911-20 (2000)
National Cancer Institute-Bethesda
Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.EBI
J Med Chem 43: 900-10 (2000)
RhôNe-Poulenc Rorer
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.BDB
J Med Chem 43: 843-58 (2000)
Parke-Davis Pharmaceutical Research
Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands.EBI
J Med Chem 43: 829-42 (2000)
National Institute Of Diabetes
Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling.EBI
J Med Chem 43: 819-28 (2000)
Salk Institute
Design of potent dicyclic (1-5/4-10) gonadotropin releasing hormone (GnRH) antagonists.EBI
J Med Chem 43: 807-18 (2000)
Salk Institute
Design of monocyclic (1-3) and dicyclic (1-3/4-10) gonadotropin releasing hormone (GnRH) antagonists.EBI
J Med Chem 43: 797-806 (2000)
Salk Institute
Design of potent dicyclic (4-10/5-8) gonadotropin releasing hormone (GnRH) antagonists.EBI
J Med Chem 43: 784-96 (2000)
Salk Institute
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.EBI
J Med Chem 43: 775-7 (2000)
Searle Research And Development
Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.EBI
J Med Chem 43: 772-4 (2000)
Georgetown University Medical Center
1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.EBI
J Med Chem 43: 769-71 (2000)
Novartis Institute For Medical Sciences
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI
J Med Chem 43: 765-8 (2000)
The R. W. Johnson Pharmaceutical Research Institute
The discovery and synthesis of highly potent, A2a receptor agonists.EBI
Bioorg Med Chem Lett 10: 403-6 (2000)
Glaxowellcome Medicines Research Centre
Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor.EBI
Bioorg Med Chem Lett 10: 399-402 (2000)
Novo Nordisk
2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2.EBI
Bioorg Med Chem Lett 10: 395-8 (2000)
Smithkline Beecham Pharmaceuticals
Mechanism-based inactivation of thymidylate synthase by 5-(3-fluoropropyn-1-yl)-2'-deoxyuridine 5'-phosphate.EBI
Bioorg Med Chem Lett 10: 391-4 (2000)
State University Of New York
Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere.EBI
Bioorg Med Chem Lett 10: 385-9 (2000)
Eli Lilly
Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.EBI
Bioorg Med Chem Lett 10: 373-5 (2000)
Sankyo
Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1.EBI
Bioorg Med Chem Lett 10: 353-6 (2000)
Università
Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA.EBI
Bioorg Med Chem Lett 10: 345-7 (2000)
Parke-Davis Neuroscience Research Centre
2-Methyladenosine-Substituted 2',5'-oligoadenylates: conformations, 2-5A binding and catalytic activities with human ribonuclease L.EBI
Bioorg Med Chem Lett 10: 329-31 (2000)
Gifu University
Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium.BDB
Eur J Pharmacol 390: 245-8 (2000)
Eli Lilly
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.EBI
Bioorg Med Chem Lett 10: 301-4 (2000)
Dupont Pharmaceuticals
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.EBI
Bioorg Med Chem Lett 10: 297-300 (2000)
Georgetown University Medical Center
Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2.EBI
Bioorg Med Chem Lett 10: 285-8 (2000)
Univ. De Valencia
Probing the extended binding determinants of oligosaccharyl transferase with synthetic inhibitors of asparagine-linked glycosylation.EBI
Bioorg Med Chem Lett 10: 281-4 (2000)
Institute Of Technology
A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 2,3-disubstituted-4-phenylquinolines.EBI
Bioorg Med Chem Lett 10: 277-9 (2000)
Searle Discovery
3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors.EBI
Bioorg Med Chem Lett 10: 273-5 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.BDB
Bioorg Med Chem Lett 10: 265-8 (2000)
Medivir
N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.EBI
Bioorg Med Chem Lett 10: 257-60 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.BDB
Bioorg Med Chem Lett 10: 253-6 (2000)
Sapienza University Of Rome
Exploring the chiral space within the active site of alpha-thrombin with a constrained mimic of D-Phe-Pro-Arg--design, synthesis, inhibitory activity, and X-ray structure of an enzyme-inhibitor complex.EBI
Bioorg Med Chem Lett 10: 243-7 (2000)
Universit£
Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.EBI
Bioorg Med Chem Lett 10: 235-8 (2000)
Merck Research Laboratories
The discovery of potent cRaf1 kinase inhibitors.EBI
Bioorg Med Chem Lett 10: 223-6 (2000)
Glaxo Wellcome
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI
Bioorg Med Chem Lett 10: 217-21 (2000)
Rhone-Poulenc Rorer
N-(sulfonamido)alkyl[tetrahydro-1H-benzo[e]indol-2-yl]amines: potent antagonists of human neuropeptide Y Y5 receptor.EBI
Bioorg Med Chem Lett 10: 213-6 (2000)
The R. W. Johnson Pharmaceutical Research Institute
Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.EBI
Bioorg Med Chem Lett 10: 209-11 (2000)
Università
Preparation of 5-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyloxy)-6-hydroxynap htho[2,3- f]quinoline-7,12-dione (FT-Alz), a new-type, potentially antitumor substance with various biological activities.EBI
Bioorg Med Chem Lett 10: 203-7 (2000)
Institute Of Bioorganic Chemistry
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.EBI
Bioorg Med Chem Lett 10: 199-201 (2000)
Kyoto Pharmaceutical University
Thermodynamics of substrate binding to the chaperone SecB.BDB
Biochemistry 39: 2420-7 (2000)
Indian Institute Of Science
5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors.BDB
Mol Pharmacol 57: 642-9 (2000)
National Institute On Drug Abuse
Dolastatin 3 and two novel cyclic peptides from a palauan collection of Lyngbya majuscula.EBI
J Nat Prod 63: 279-82 (2000)
University Of California At San Diego
Cernuosides A and B, two sucrase inhibitors from Pulsatilla cernua.EBI
J Nat Prod 63: 276-8 (2000)
China Pharmaceutical University
Inhibitory effects on HIV-1 protease of constituents from the wood of Xanthoceras sorbifolia.EBI
J Nat Prod 63: 238-42 (2000)
Toyama Medical And Pharmaceutical University
Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.EBI
J Med Chem 43: 756-62 (2000)
Friedrich-Alexander University
Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.EBI
J Med Chem 43: 721-35 (2000)
Searle Research And Development
A new class of conformationally rigid analogues of 4-amino-5-halopentanoic acids, potent inactivators of gamma-aminobutyric acid aminotransferase.EBI
J Med Chem 43: 706-20 (2000)
Northwestern University
Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.EBI
J Med Chem 43: 690-705 (2000)
Abbott Laboratories
Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: first phosphodiesterase 7 inhibitors.EBI
J Med Chem 43: 683-9 (2000)
Instituto De QuíMica MéDica
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.EBI
J Med Chem 43: 675-82 (2000)
Novartis Pharma
Inhibitors of tripeptidyl peptidase II. 2. Generation of the first novel lead inhibitor of cholecystokinin-8-inactivating peptidase: a strategy for the design of peptidase inhibitors.EBI
J Med Chem 43: 664-74 (2000)
University College London
Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography.EBI
J Med Chem 43: 639-48 (2000)
Emory University
Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.EBI
J Med Chem 43: 599-608 (2000)
Universit£
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.BDB
J Med Chem 43: 581-90 (2000)
University Of Tennessee At Memphis
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.EBI
J Med Chem 43: 569-80 (2000)
University Of Arizona
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.EBI
J Med Chem 43: 551-9 (2000)
Clinical Research Institute Of Montr£Al
The PPARs: from orphan receptors to drug discovery.EBI
J Med Chem 43: 527-50 (2000)
Glaxo Wellcome Research & Development
Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).EBI
J Pharmacol Exp Ther 292: 1146-52 (2000)
University Of California
Cloning and pharmacological characterization of the rat CB(2) cannabinoid receptor.BDB
J Pharmacol Exp Ther 292: 886-94 (2000)
Virginia Commonwealth University
Interactions of HIV protease inhibitors with a human organic cation transporter in a mammalian expression system.EBI
Drug Metab Dispos 28: 329-34 (2000)
University Of California
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.EBI
Bioorg Med Chem Lett 10: 193-5 (2000)
Dupont Pharmaceuticals
8-Aminocyclazocine analogues: synthesis and structure-activity relationships.EBI
Bioorg Med Chem Lett 10: 183-7 (2000)
Institute
RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.EBI
Bioorg Med Chem Lett 10: 179-82 (2000)
Hoechst Marion Roussel
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.EBI
Bioorg Med Chem Lett 10: 175-8 (2000)
Synaptic Pharmaceutical
Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.EBI
Bioorg Med Chem Lett 10: 167-70 (2000)
Astrazeneca R&D MontréAl
The flavanolignan silybin and its hemisynthetic derivatives, a novel series of potential modulators of P-glycoprotein.EBI
Bioorg Med Chem Lett 10: 157-60 (2000)
Universit£
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.EBI
Bioorg Med Chem Lett 10: 147-51 (2000)
Wyeth-Ayerst Research
First enantiospecific synthesis of a 3,4-dihydroxy-L-glutamic acid [(3S,4S)-DHGA], a new mGluR1 agonist.EBI
Bioorg Med Chem Lett 10: 129-33 (2000)
Cnrs
New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.EBI
J Med Chem 43: 517-25 (2000)
University Of Groningen
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.EBI
J Med Chem 43: 488-504 (2000)
Novartis Institute For Biomedical Research
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.EBI
J Med Chem 43: 449-56 (2000)
Dupont Pharmaceuticals
Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.EBI
J Med Chem 43: 440-8 (2000)
University Of WüRzburg
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.EBI
J Med Chem 43: 432-9 (2000)
University Of Groningen
Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca(2+)-activated K(+) channel.EBI
J Med Chem 43: 420-31 (2000)
University College London
Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.EBI
J Med Chem 43: 409-19 (2000)
Eisai
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.EBI
J Med Chem 43: 401-8 (2000)
Mayo Medical School And Mayo Clinic
Derivation of pharmacophore and CoMFA models for leukotriene D(4) receptor antagonists of the quinolinyl(bridged)aryl series.EBI
J Med Chem 43: 392-400 (2000)
Laboratorios Menarini
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.EBI
J Med Chem 43: 381-91 (2000)
University Of Minnesota
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.EBI
J Med Chem 43: 369-80 (2000)
Procter And Gamble Pharmaceuticals
Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.EBI
J Med Chem 43: 361-8 (2000)
Warner-Lambert
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies.EBI
J Med Chem 43: 351-60 (2000)
Georgetown University Medical Center
alpha-Substituted N-(sulfonamido)alkyl-beta-aminotetralins: potent and selective neuropeptide Y Y5 receptor antagonists.EBI
J Med Chem 43: 346-50 (2000)
The R. W. Johnson Pharmaceutical Research Institute
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).BDB
J Med Chem 43: 342-5 (2000)
Smithkline Beecham Pharmaceuticals
Protease inhibitors: current status and future prospects.EBI
J Med Chem 43: 305-41 (2000)
University Of Queensland
Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.BDB
Chem Biol 7: 27-38 (2000)
University Of California San Francisco
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.BDB
Bioorg Med Chem 7: 2775-800 (1999)
Parke-Davis Pharmaceutical Research
DNA polymerase beta inhibitors from Tetracera boiviniana.EBI
J Nat Prod 62: 1660-3 (2000)
University Of Virginia
DNA polymerase beta inhibitors from Baeckea gunniana.EBI
J Nat Prod 62: 1624-6 (2000)
University Of Virginia
Dimerization of resveratrol by the grapevine pathogen Botrytis cinerea.EBI
J Nat Prod 63: 29-33 (2000)
University Of Louisiana At Monroe
Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes.EBI
J Med Chem 43: 292-300 (2000)
Università
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.EBI
J Med Chem 43: 270-7 (2000)
Universitá
N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.EBI
J Med Chem 43: 250-60 (2000)
Universit£
Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.EBI
J Med Chem 43: 236-49 (2000)
Novartis Institute For Biomedical Research
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.EBI
J Med Chem 43: 214-23 (2000)
RhôNe-Poulenc Rorer
Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.EBI
J Med Chem 43: 205-13 (2000)
Massachusetts General Hospital
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.EBI
J Med Chem 43: 177-89 (2000)
Otsuka Pharmaceutical
Antitumor agents. 199. Three-dimensional quantitative structure-activity relationship study of the colchicine binding site ligands using comparative molecular field analysis.EBI
J Med Chem 43: 167-76 (2000)
University Of North Carolina At Chapel Hill
Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.EBI
J Med Chem 43: 156-66 (2000)
Parke-Davis Pharmaceutical Research
Synthesis and pharmacological characterization of [(125)I]iodomethyllycaconitine ([(125)I]iodo-MLA). A new ligand for the alpha(7) nicotinic acetylcholine receptor.EBI
J Med Chem 43: 142-5 (2000)
Research Triangle Institute
Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.EBI
J Med Chem 43: 139-41 (2000)
University Of Bristol
Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver.EBI
Gastroenterology 118: 422-30 (2000)
University Hospital
Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.BDB
J Neurochem 74: 478-89 (2000)
Janssen Research Foundation
A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.EBI
Am J Physiol Gastrointest Liver Physiol 278: 156-64 (2000)
Deutsches Krebsforschungszentrum
Synthesis and biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization.EBI
J Med Chem 42: 5475-81 (2000)
University Of Antwerp
Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.BDB
J Med Chem 42: 5464-74 (1999)
Parke-Davis Pharmaceutical Research
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.EBI
J Med Chem 42: 5455-63 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships.EBI
J Med Chem 42: 5448-54 (2000)
Heidelberg University
2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.EBI
J Med Chem 42: 5437-47 (2000)
University Of Leipzig
Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.EBI
J Med Chem 42: 5426-36 (2000)
University Of Florida
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.EBI
J Med Chem 42: 5415-25 (2000)
Berlex Biosciences
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.EBI
J Med Chem 42: 5390-401 (2000)
Universit¿A Di Perugia
Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.BDB
J Med Chem 42: 5369-89 (1999)
Astrazeneca
Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.EBI
J Med Chem 42: 5359-68 (2000)
The University Of Arizona
Molecular recognition of modified adenine nucleotides by the P2Y(1)-receptor. 1. A synthetic, biochemical, and NMR approach.EBI
J Med Chem 42: 5325-37 (2000)
Bar-Ilan University
Synthesis and structure-activity relationships of new 1, 3-disubstituted cyclohexanes as structurally rigid leukotriene B(4) receptor antagonists.EBI
J Med Chem 42: 5289-310 (1999)
Cnrs 5074
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.BDB
Proc Natl Acad Sci U S A 97: 925-30 (2000)
Vanderbilt University School Of Medicine
beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter.EBI
J Biol Chem 275: 1699-707 (2000)
Medical College Of Georgia
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.EBI
Bioorg Med Chem Lett 10: 87-90 (2000)
Institute
Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.EBI
Bioorg Med Chem Lett 10: 83-5 (2000)
3-Dimensional Pharmaceuticals
Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor.EBI
Bioorg Med Chem Lett 10: 79-82 (2000)
3-Dimensional Pharmaceuticals
Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.EBI
Bioorg Med Chem Lett 10: 75-8 (2000)
University Hospital Zurich
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.EBI
Bioorg Med Chem Lett 10: 71-4 (2000)
Janssen Research Foundation
Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of 2-alkylated benzolactams.EBI
Bioorg Med Chem Lett 10: 63-6 (2000)
University Of Tokyo
Synthesis and binding studies of some epibatidine analogues.EBI
Bioorg Med Chem Lett 10: 55-8 (2000)
Institute Of Pharmacy And Biochemistry
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.EBI
Bioorg Med Chem Lett 10: 35-8 (2000)
Institut De Recherche Jouveinal-Parke Davis
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.EBI
Bioorg Med Chem Lett 10: 31-4 (2000)
Chembridge
Binding dynamics of two water molecules constrained within the scytalone dehydratase binding pocket.EBI
Bioorg Med Chem Lett 10: 23-6 (2000)
Fmc Stine Research Center
A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.EBI
Bioorg Med Chem Lett 10: 17-8 (2000)
University Of Maryland
Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence.EBI
Bioorg Med Chem Lett 10: 13-6 (2000)
Cor Therapeutics
Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.EBI
Bioorg Med Chem Lett 10: 5-8 (2000)
Merck Research Laboratories
Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.EBI
Bioorg Med Chem Lett 10: 1-4 (2000)
3-Dimensional Pharmaceuticals
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.BDB
Biochim Biophys Acta 1483: 285-93 (2000)
Merck Frosst Centre For Therapeutic Research
Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase.EBI
J Med Chem 43: 133-8 (2000)
Glaxo Wellcome
Synthesis and SAR of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids and esters and 2-amino-4-aryl-4-oxobut-2-enoic acids and esters: potent inhibitors of kynurenine-3-hydroxylase as potential neuroprotective agents.EBI
J Med Chem 43: 123-7 (2000)
Glaxo Wellcome Research And Development
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.EBI
J Med Chem 43: 114-22 (2000)
Harvard Medical School
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.EBI
J Med Chem 43: 71-95 (2000)
University Of Wisconsin-Milwaukee
QSAR analysis of Delta(8)-THC analogues: relationship of side-chain conformation to cannabinoid receptor affinity and pharmacological potency.EBI
J Med Chem 43: 59-70 (2000)
Research Triangle Institute
Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).EBI
J Med Chem 43: 41-58 (2000)
Dupont Pharmaceuticals
Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).EBI
J Med Chem 43: 27-40 (2000)
Dupont Pharmaceuticals
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.EBI
J Med Chem 43: 22-6 (2000)
Smithkline Beecham Pharmaceuticals
Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.EBI
J Med Chem 43: 19-21 (2000)
Glaxo Wellcome Research And Development
Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities.BDB
Bioorg Med Chem 7: 2569-75 (1999)
Hong Kong University Of Science And Technology
Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.BDB
Bioorg Med Chem 7: 2487-97 (1999)
University Of Alabama At Birmingham
Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine.BDB
Mol Pharmacol 57: 75-81 (2000)
Dupont Pharmaceuticals
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.EBI
Bioorg Med Chem Lett 9: 3459-64 (2000)
Corvas International
Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.EBI
Bioorg Med Chem Lett 9: 3441-6 (2000)
University Of Louisville
Delta opioid binding selectivity of 3-ether analogs of naltrindole.EBI
Bioorg Med Chem Lett 9: 3435-8 (2000)
National Institute Of Diabetes
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.EBI
Bioorg Med Chem Lett 9: 3411-6 (2000)
Institute
Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.EBI
Bioorg Med Chem Lett 9: 3397-402 (1999)
The University Of Tokyo
Reversal of resistance in multidrug resistance protein (MRP1)-overexpressing cells by LY329146.EBI
Bioorg Med Chem Lett 9: 3381-6 (2000)
Eli Lilly
Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.EBI
Bioorg Med Chem Lett 9: 3375-80 (2000)
University Of Illinois At Chicago
4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines: selective h5-HT1D agonists for the treatment of migraine.EBI
Bioorg Med Chem Lett 9: 3369-74 (2000)
Merck Sharp & Dohme Research Laboratories
First fatty acylated dipeptides to affect muscarinic receptor ligand binding.EBI
Bioorg Med Chem Lett 9: 3363-8 (2000)
University Of Toledo
4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI
Bioorg Med Chem Lett 9: 3351-6 (2000)
Celltech Therapeutics
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.EBI
Bioorg Med Chem Lett 9: 3347-50 (2000)
Research Triangle Institute
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.EBI
Bioorg Med Chem Lett 9: 3329-34 (2000)
Glaxo Wellcome Research And Development
N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.EBI
Bioorg Med Chem Lett 9: 3325-8 (2000)
Georgetown University Medical Center
Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.EBI
Bioorg Med Chem Lett 9: 3307-12 (2000)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.EBI
Bioorg Med Chem Lett 9: 3301-6 (2000)
Merck Research Laboratories
Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.EBI
Bioorg Med Chem Lett 9: 3285-90 (2000)
Yoshitomi Pharmaceutical Industries
Synthesis and acetylcholinesterase inhibitory activity of huperzine A-E2020 combined compound.EBI
Bioorg Med Chem Lett 9: 3279-84 (2000)
Institute Of Materia Medica
Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.EBI
Bioorg Med Chem Lett 9: 3273-6 (2000)
University Of New Orleans
Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry.EBI
Bioorg Med Chem Lett 9: 3267-72 (2000)
University Of California
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.BDB
Synapse 35: 144-50 (2000)
Albany Medical College
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.BDB
Synapse 35: 79-95 (2000)
Institut De Recherches Servier
Equilibrium thermodynamics of a physiologically-relevant heme-protein complex.BDB
Biochemistry 38: 16876-81 (1999)
University Of North Carolina At Chapel Hill
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.BDB
J Pharmacol Exp Ther 292: 215-27 (2000)
University Of Colorado
Vasorelaxation by new hybrid compounds containing dihydropyridine and pinacidil-like moieties.EBI
J Med Chem 42: 5266-71 (1999)
National Academy Of Sciences Of Ukraine
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.EBI
J Med Chem 42: 5254-65 (2000)
The R. W. Johnson Pharmaceutical Research Institute
Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.EBI
J Med Chem 42: 5241-53 (2000)
Bristol-Myers Squibb Pharmaceutical Research Institute
Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme.EBI
J Med Chem 42: 5197-211 (2000)
University Of Paris
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.EBI
J Med Chem 42: 5181-7 (2000)
Warner-Lambert
Simple linear QSAR models based on quantum similarity measures.EBI
J Med Chem 42: 5169-80 (2000)
Czech Academy Of Sciences
Binding constants of neuraminidase inhibitors: An investigation of the linear interaction energy method.EBI
J Med Chem 42: 5142-52 (2000)
University Of Southampton
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.BDB
J Med Chem 42: 5120-30 (1999)
Sugen
Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.EBI
J Med Chem 42: 5077-94 (2000)
Wyeth-Ayerst Research
Alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles.EBI
J Med Chem 42: 5064-71 (1999)
The R. W. Johnson Pharmaceutical Research Institute
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).EBI
J Med Chem 42: 5061-3 (2000)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.BDB
Naunyn Schmiedebergs Arch Pharmacol 360: 488-99 (1999)
Novartis Pharma
Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.BDB
Eur J Pharmacol 383: 209-14 (1999)
Hungarian Academy Of Sciences
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.EBI
J Med Chem 42: 5029-42 (2000)
National Institute Of Diabetes And Digestive And Kidney Diseases
Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT(3) receptors.EBI
J Med Chem 42: 5020-8 (2000)
Universidad Complutense
Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism.EBI
J Med Chem 42: 5010-9 (2000)
University Of Ferrara
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.EBI
J Med Chem 42: 4981-5001 (2000)
Merck Sharp & Dohme Research Laboratories
Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling.EBI
J Med Chem 42: 4970-80 (1999)
Novo Nordisk
Structure-activity relationship studies of novel heteroretinoids: induction of apoptosis in the HL-60 cell line by a novel isoxazole-containing heteroretinoid.EBI
J Med Chem 42: 4961-9 (2000)
Università
On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists.EBI
J Med Chem 42: 4952-60 (2000)
Polish Academy Of Sciences
Kainate receptors are involved in synaptic plasticity.BDB
Nature 402: 297-301 (1999)
University Of Bristol
Anti-HIV-1 protease triterpenoid saponins from the seeds of Aesculus chinensis.EBI
J Nat Prod 62: 1510-3 (1999)
Beijing Medical University
Synthesis and biological evaluation of a potent E-selectin antagonist.EBI
J Med Chem 42: 4909-13 (1999)
Novartis Pharma
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.EBI
J Med Chem 42: 4890-908 (1999)
Astrazeneca
Fused bicyclic Gly-Asp beta-turn mimics with specific affinity for GPIIb-IIIa.EBI
J Med Chem 42: 4875-89 (1999)
Eli Lilly
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.BDB
J Med Chem 42: 4861-74 (1999)
Purdue University
Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.EBI
J Med Chem 42: 4853-60 (1999)
Harvard Medical School
Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.EBI
J Med Chem 42: 4844-52 (1999)
Abbott Laboratories
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.EBI
J Med Chem 42: 4836-43 (1999)
Georgia Institute Of Technology
Synthesis, acid-base behavior, and binding properties of 6-modified myo-inositol 1,4,5-tris(phosphate)s.EBI
J Med Chem 42: 4824-35 (1999)
Laboratoire De Pharmacochimie De La Communication Cellulaire Umr 7081 Du Cnrs
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.EBI
J Med Chem 42: 4804-13 (1999)
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.EBI
J Med Chem 42: 4794-803 (1999)
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.EBI
J Med Chem 42: 4778-93 (1999)
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.EBI
J Med Chem 42: 4764-77 (1999)
Synaptic Pharmaceutical
Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors.EBI
J Med Chem 42: 4729-32 (1999)
Martin-Luther-University Halle-Wittenberg
Inhibition and substrate activity of conformationally rigid vigabatrin analogues with gamma-aminobutyric acid aminotransferase.EBI
J Med Chem 42: 4725-8 (1999)
Northwestern University
Discovery of novel non-peptide CCR1 receptor antagonists.EBI
J Med Chem 42: 4680-94 (1999)
Berlex Biosciences
Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.EBI
J Med Chem 42: 4669-79 (1999)
WestfäLische Wilhelms-UniversitäT MüNster
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.EBI
J Med Chem 42: 4659-68 (1999)
Insituto De Qu�Mica M�Dica (Csic)
Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth.EBI
J Med Chem 42: 4630-9 (1999)
University Of Nebraska Medical Center
Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.EBI
J Med Chem 42: 4621-9 (1999)
Research Triangle Institute
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.EBI
J Med Chem 42: 4584-603 (1999)
Novartis Horsham Research Centre
Specific nonpeptide photoprobes as tools for the structural study of the angiotensin II AT(1) receptor.EBI
J Med Chem 42: 4572-83 (1999)
Laboratoires Fournier
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.EBI
J Med Chem 42: 4547-62 (1999)
Procter And Gamble Pharmaceuticals
Molecular modeling studies on G-quadruplex complexes of telomerase inhibitors: structure-activity relationships.EBI
J Med Chem 42: 4538-46 (1999)
The Institute Of Cancer Research
Angiotensin II analogues encompassing 5,9- and 5,10-fused thiazabicycloalkane tripeptide mimetics.EBI
J Med Chem 42: 4524-37 (1999)
Uppsala University
Affinity and selectivity of matrix metalloproteinase inhibitors: a chemometrical study from the perspective of ligands and proteins.EBI
J Med Chem 42: 4506-23 (1999)
Hoechst Marion Roussel
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.EBI
J Med Chem 42: 4473-8 (1999)
Università
Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2.EBI
Br J Pharmacol 128: 1159-64 (1999)
Kyoto University Hospital
Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.EBI
Bioorg Med Chem Lett 9: 3243-8 (1999)
Merck
Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.EBI
Bioorg Med Chem Lett 9: 3225-30 (1999)
Merck Research Laboratories
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).BDB
Bioorg Med Chem Lett 9: 3221-4 (1999)
Dupont Pharmaceuticals
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.EBI
Bioorg Med Chem Lett 9: 3217-20 (1999)
Dupont Pharmaceuticals
Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.EBI
Bioorg Med Chem Lett 9: 3211-6 (1999)
Georgetown University Medical Center
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.EBI
Bioorg Med Chem Lett 9: 3187-92 (1999)
Merck Frosst Centre For Therapeutic Research
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 9: 3181-6 (1999)
Merck Frosst Centre For Therapeutic Research
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.EBI
Bioorg Med Chem Lett 9: 3053-6 (1999)
Research Triangle Institute
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.EBI
Bioorg Med Chem Lett 9: 3031-4 (1999)
Dipartimento Di Scienze Farmaceutiche - Università
Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.EBI
Bioorg Med Chem Lett 9: 3009-14 (1999)
Ariad Pharmaceuticals
A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects.EBI
Bioorg Med Chem Lett 9: 2999-3002 (1999)
Institute For Bio-Medical Research
Synthesis and biological characterization of sqbazide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A2 receptor.EBI
Bioorg Med Chem Lett 9: 2963-8 (1999)
Ecole Nationale SupéRieure De Chimie De Paris
Guanidine-substituted imidazoles as inhibitors of nitric oxide synthase.EBI
Bioorg Med Chem Lett 9: 2953-8 (1999)
Wake Forest University Winston-Salem
Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids.EBI
Bioorg Med Chem Lett 9: 2915-20 (1999)
Novartis Pharma
3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.EBI
Bioorg Med Chem Lett 9: 2909-14 (1999)
Seoul National University
Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate.EBI
Mol Pharmacol 56: 1254-61 (1999)
Bayerische Julius-Maximilians-Universit£T
Effect of multidrug resistance-reversing agents on transporting activity of human canalicular multispecific organic anion transporter.EBI
Mol Pharmacol 56: 1219-28 (1999)
Kagoshima University
Characterization and function of the bovine kidney epithelial angiotensin receptor subtype 4 using angiotensin IV and divalinal angiotensin IV as receptor ligands.BDB
J Pharmacol Exp Ther 291: 1242-9 (1999)
Washington State University
Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.EBI
J Pharmacol Exp Ther 291: 1204-9 (1999)
Vanderbilt University School Of Medicine
Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.BDB
J Pharmacol Exp Ther 291: 1093-9 (1999)
Loughborough University
Revised structure of a homonojirimycin isomer from Aglaonema treubii: first example of a naturally occurring alpha-homoallonojirimycin.EBI
Bioorg Med Chem Lett 9: 3171-4 (1999)
Institut De Chimie Organique Et Analytique (I.C.O.A.)
Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents.EBI
Bioorg Med Chem Lett 9: 3165-70 (1999)
Smithkline Beecham Pharmaceuticals
3-Amidinophenylalanine-based inhibitors of urokinase.EBI
Bioorg Med Chem Lett 9: 3147-52 (1999)
UniversitäT Jena
Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.EBI
Bioorg Med Chem Lett 9: 3143-6 (1999)
Friedrich-Alexander University
The inhibition of human cytomegalovirus (hCMV) protease by hydroxylamine derivatives.EBI
Bioorg Med Chem Lett 9: 3137-42 (1999)
Smithkline Beecham Pharmaceuticals
4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists.EBI
Bioorg Med Chem Lett 9: 3103-8 (1999)
The James Black Foundation
Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.EBI
Bioorg Med Chem Lett 9: 3093-8 (1999)
The University Of Sydney
Isolation of xestosterol esters of brominated acetylenic fatty acids from the marine sponge xestospongia testudinariaEBI
J Nat Prod 62: 1439-42 (1999)
Griffith University
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.EBI
J Med Chem 42: 4462-70 (1999)
Universita' Degli Studi Di Salerno
Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.EBI
J Med Chem 42: 4456-61 (1999)
Abbott Laboratories
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.EBI
J Med Chem 42: 4446-55 (1999)
National Institute On Drug Abuse-Intramural Research Program
Heteroarotinoids inhibit head and neck cancer cell lines in vitro and in vivo through both RAR and RXR retinoic acid receptors.EBI
J Med Chem 42: 4434-45 (1999)
University Of Oklahoma Health Sciences Center
Two-stage method for protein-ligand docking.EBI
J Med Chem 42: 4422-33 (1999)
German National Research Center For Information Technology
Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.EBI
J Med Chem 42: 4394-404 (1999)
Université
Compounds that activate the mouse melanocortin-1 receptor identified by screening a small molecule library based upon the beta-turn.EBI
J Med Chem 42: 4380-7 (1999)
Oregon Health Sciences University
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.EBI
J Med Chem 42: 4362-79 (1999)
Universita' Degli Studi Di Salerno
Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.EBI
J Med Chem 42: 4351-61 (1999)
University Of Kansas
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.EBI
J Med Chem 42: 4331-42 (1999)
Uppsala University
Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.EBI
J Med Chem 42: 4300-12 (1999)
Cardiff University
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.EBI
J Med Chem 42: 4281-91 (1999)
Novo Nordisk
Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor.BDB
J Biol Chem 274: 31272-8 (1999)
Indian Institute Of Science
Structure-activity relationship of HIV-1 protease inhibitors containing alpha-hydroxy-beta-amino acids. Detailed study of P1 site.BDB
Bioorg Med Chem 7: 2063-72 (1999)
Sankyo
Recognition of L-amino acid ester compounds by rat peptide transporters PEPT1 and PEPT2.EBI
J Pharmacol Exp Ther 291: 705-9 (1999)
Kyoto University Hospital
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.EBI
Bioorg Med Chem Lett 9: 2887-92 (1999)
British Biotech Pharmaceuticals
2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.EBI
Bioorg Med Chem Lett 9: 2863-6 (1999)
Glaxowellcome Medicines Research Centre
Interaction of tyrosyl aryl dipeptides with S. aureus tyrosyl tRNA synthetase: inhibition and crystal structure of a complex.EBI
Bioorg Med Chem Lett 9: 2859-62 (1999)
Smithkline Beecham Pharmaceuticals
Design and synthesis of novel dihydropyridine alpha-1a antagonists.EBI
Bioorg Med Chem Lett 9: 2843-8 (1999)
Synaptic Pharmaceutical
Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.EBI
Bioorg Med Chem Lett 9: 2837-42 (1999)
Nv Organon
Synthesis and biological evaluation of 1,1-difluoro-2-(tetrahydro-3-furanyl)ethylphosphonic acids possessing a N9-purinylmethyl functional group at the ring. a new class of inhibitors for purine nucleoside phosphorylases.EBI
Bioorg Med Chem Lett 9: 2833-6 (1999)
Tokyo University Of Pharmacy & Life Science
Design, combinatorial chemical synthesis and in vitro characterization of novel urea based gelatinase inhibitors.EBI
Bioorg Med Chem Lett 9: 2823-6 (1999)
University Of Wisconsin-Madison
Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.EBI
Bioorg Med Chem Lett 9: 2819-22 (1999)
Korea Research Institute Of Chemical Technology
Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.EBI
Bioorg Med Chem Lett 9: 2815-8 (1999)
Warner-Lambert
Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity.BDB
Bioorg Med Chem Lett 9: 2811-4 (1999)
Gilead Sciences
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.BDB
Bioorg Med Chem Lett 9: 2805-10 (1999)
Dupont Pharmaceuticals
The synthesis of a new class of oxytocin antagonists.EBI
Bioorg Med Chem Lett 9: 2801-4 (1999)
Ferring Research Institute
Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.EBI
Bioorg Med Chem Lett 9: 2795-800 (1999)
Institute Of Science And Technology
Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.EBI
J Nat Prod 62: 1241-5 (1999)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity.EBI
J Med Chem 42: 4269-74 (1999)
Freie UniversitäT Berlin
Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain.EBI
J Med Chem 42: 4257-63 (1999)
Purdue University
3-Alkyl-6-chloro-2-pyrones: selective inhibitors of pancreatic cholesterol esterase.EBI
J Med Chem 42: 4250-6 (1999)
University Of New Mexico
Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties.EBI
J Med Chem 42: 4239-49 (1999)
Warner-Lambert
Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.EBI
J Med Chem 42: 4232-8 (1999)
National Institute Of Diabetes
Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.BDB
J Med Chem 42: 4225-31 (1999)
Hong Kong University Of Science And Technology
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.EBI
J Med Chem 42: 4214-24 (1999)
University Of Bologna
Synthesis and characterization of bradykinin B(2) receptor agonists containing constrained dipeptide mimics.EBI
J Med Chem 42: 4193-201 (1999)
University Of Montpellier
Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.EBI
J Med Chem 42: 4185-92 (1999)
University Of Montpellier
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.BDB
J Med Chem 42: 4150-60 (1999)
Medivir
Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.EBI
J Med Chem 42: 4140-9 (1999)
Pharmacia & Upjohn
Protein kinase C ligands based on tetrahydrofuran templates containing a new set of phorbol ester pharmacophores.EBI
J Med Chem 42: 4129-39 (1999)
Seoul National University
Inhibition of neuronal nitric oxide synthase by 4-amino pteridine derivatives: structure-activity relationship of antagonists of (6R)-5,6,7,8-tetrahydrobiopterin cofactor.EBI
J Med Chem 42: 4108-21 (1999)
Julius-Maximilians University WüRzburg
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70.BDB
J Med Chem 42: 4088-98 (1999)
Ariad Pharmaceuticals
Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.EBI
J Med Chem 42: 4081-7 (1999)
University Of North Carolina At Chapel Hill
Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains.EBI
J Med Chem 42: 4054-61 (1999)
Uppsala University
Diethylcarbamoylating/nitroxylating agents as dual action inhibitors of aldehyde dehydrogenase: a disulfiram-cyanamide merger.EBI
J Med Chem 42: 4016-20 (1999)
Va Medical Center
Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.EBI
Bioorg Med Chem Lett 9: 2773-8 (1999)
Pfizer
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.EBI
Bioorg Med Chem Lett 9: 2763-6 (1999)
University Of Arizona
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI
Bioorg Med Chem Lett 9: 2753-8 (1999)
RhôNe-Poulenc Rorer
Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.EBI
Bioorg Med Chem Lett 9: 2747-52 (1999)
Abbott Laboratories
Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.EBI
Bioorg Med Chem Lett 9: 2741-6 (1999)
Merck Research Laboratories
9-[(2'S,3'S)-3'-formyl-2',3'-dihydroxypropyl]adenine: a facile affinity-labeling probe of human S-adenosyl-L-homocysteine hydrolase.EBI
Bioorg Med Chem Lett 9: 2737-40 (1999)
Gifu University
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.EBI
Bioorg Med Chem Lett 9: 2721-6 (1999)
Institute
Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.EBI
Bioorg Med Chem Lett 9: 2715-20 (1999)
Smithkline Beecham Pharmaceuticals
New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.EBI
Bioorg Med Chem Lett 9: 2699-704 (1999)
Merck Frosst Centre For Therapeutic Research
Syntheses of novel antitumor dihydroxanthone derivatives with inhibitory activity against DNA topoisomerase II.EBI
Bioorg Med Chem Lett 9: 2653-6 (1999)
Ajinomoto
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.EBI
J Med Chem 42: 4001-9 (1999)
Brown University
Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.EBI
J Med Chem 42: 3982-93 (1999)
Takeda Chemical Industries
Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.EBI
J Med Chem 42: 3971-81 (1999)
Anormed
Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.EBI
J Med Chem 42: 3965-70 (1999)
Taisho Pharmaceutical
Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.EBI
J Med Chem 42: 3934-41 (1999)
Universit£
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.EBI
J Med Chem 42: 3910-8 (1999)
Washington University
Substituted isoquinolines and quinazolines as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha.EBI
J Med Chem 42: 3860-73 (1999)
University Of California
Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.EBI
J Med Chem 42: 3852-9 (1999)
Abbott Laboratories
Design and fast synthesis of C-terminal duplicated potent C(2)-symmetric P1/P1'-modified HIV-1 protease inhibitors.BDB
J Med Chem 42: 3835-44 (1999)
Uppsala University
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.EBI
J Med Chem 42: 3809-20 (1999)
Astrazeneca
Novel farnesol and geranylgeraniol analogues: A potential new class of anticancer agents directed against protein prenylation.EBI
J Med Chem 42: 3800-8 (1999)
Parke-Davis Pharmaceutical Research
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.EBI
J Med Chem 42: 3785-8 (1999)
Glaxo Wellcome Research & Development
N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.EBI
J Med Chem 42: 3779-84 (1999)
Merck Research Laboratories
Mixture-based synthetic combinatorial libraries.EBI
J Med Chem 42: 3743-78 (1999)
Torrey Pines Institute For Molecular Studies
The cloned guinea pig neuropeptide Y receptor Y1 conforms to other mammalian Y1 receptors.BDB
Peptides 20: 1043-53 (1999)
Uppsala University
Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells.BDB
Br J Pharmacol 128: 13-20 (1999)
Cerebrus
Asymmetric synthesis of novel quaternary alpha-hydroxy-delta-lactam dipeptide surrogates.EBI
Bioorg Med Chem Lett 9: 2625-8 (1999)
Corvas International
Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists.EBI
Bioorg Med Chem Lett 9: 2621-4 (1999)
Merck Research Laboratories
Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.EBI
Bioorg Med Chem Lett 9: 2615-20 (1999)
Merck Research Laboratories
Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transport system.EBI
Bioorg Med Chem Lett 9: 2607-12 (1999)
The University Of Montana
New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.EBI
Bioorg Med Chem Lett 9: 2593-8 (1999)
Wyeth-Ayerst Research Laboratories
Preparation and receptor binding affinities of cyclic C-terminal neurotensin (8-13) and (9-13) analogues.EBI
Bioorg Med Chem Lett 9: 2579-82 (1999)
Medical University Of South Carolina
Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI
Bioorg Med Chem Lett 9: 2573-8 (1999)
Corvas International
A new class of selective and potent inhibitors of neuronal nitric oxide synthase.EBI
Bioorg Med Chem Lett 9: 2569-72 (1999)
Pfizer
Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.EBI
Bioorg Med Chem Lett 9: 2561-4 (1999)
University Of Tokyo
Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-beta-lactamase.EBI
Bioorg Med Chem Lett 9: 2549-54 (1999)
Merck Research Laboratorie
Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.EBI
Bioorg Med Chem Lett 9: 2539-44 (1999)
Rh£Ne-Poulenc Rorer
Dysidiolide and related gamma-hydroxy butenolide compounds as inhibitors of the protein tyrosine phosphatase, CDC25.EBI
Bioorg Med Chem Lett 9: 2537-8 (1999)
Mitotix
Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.EBI
Bioorg Med Chem Lett 9: 2531-6 (1999)
Bayer
Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.EBI
Bioorg Med Chem Lett 9: 2521-4 (1999)
Pharmacia & Upjohn
A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry.EBI
Bioorg Med Chem Lett 9: 2509-14 (1999)
Fmc Stine Research Center
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.EBI
Bioorg Med Chem Lett 9: 2503-8 (1999)
Warner-Lambert
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.EBI
Bioorg Med Chem Lett 9: 2497-502 (1999)
Warner-Lambert
2,7-diazabicyclo[3.3.0]octanes as novel h5-HT receptor agonists.EBI
Bioorg Med Chem Lett 9: 2491-6 (1999)
Merck Sharp & Dohme Research Laboratories
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.EBI
Bioorg Med Chem Lett 9: 2483-6 (1999)
Biotech Research Institute
Human telomerase inhibition by substituted acridine derivatives.EBI
Bioorg Med Chem Lett 9: 2463-8 (1999)
The Institute Of Cancer Research
Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.BDB
Mol Pharmacol 56: 705-13 (1999)
University Of Virginia
2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors.BDB
Naunyn Schmiedebergs Arch Pharmacol 360: 103-8 (1999)
Universitat Wurzburg
Cloning of mouse prostaglandin transporter PGT cDNA: species-specific substrate affinities.EBI
Am J Physiol 277: 734-41 (1999)
Albert Einstein College Of Medicine
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.BDB
Bioorg Med Chem 7: 1743-54 (1999)
Otsuka Pharmaceutical
Salt links dominate affinity of antibody HyHEL-5 for lysozyme through enthalpic contributions.BDB
J Biol Chem 274: 26838-42 (1999)
University Of Houston
Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.EBI
J Nat Prod 62: 1208-11 (1999)
Harbor Branch Oceanographic Institution
DNA polymerase beta inhibitors from Sandoricum koetjape.EBI
J Nat Prod 62: 1110-3 (1999)
University Of Virginia Charlottesville
Small peptides containing phosphotyrosine and adjacent alphaMe-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain.EBI
J Med Chem 42: 3737-41 (1999)
University Of Paris
Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.EBI
J Med Chem 42: 3718-25 (1999)
Warner-Lambert
Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.EBI
J Med Chem 42: 3701-10 (1999)
Abbott Laboratories
Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route.EBI
J Med Chem 42: 3690-700 (1999)
Universit£
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.EBI
J Med Chem 42: 3679-89 (1999)
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.EBI
J Med Chem 42: 3668-78 (1999)
Abbott Laboratories
Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors.EBI
J Med Chem 42: 3647-56 (1999)
Massachusetts General Hospital
2-thioether 5'-O-(1-thiotriphosphate)adenosine derivatives as new insulin secretagogues acting through P2Y-Receptors.EBI
J Med Chem 42: 3636-46 (1999)
Bar-Ilan University
Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.EBI
J Med Chem 42: 3629-35 (1999)
Leiden/Amsterdam Center For Drug Research
Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.EBI
J Med Chem 42: 3615-22 (1999)
Max-Planck Research Unit
Synthesis, structure-activity relationships, and RARgamma-ligand interactions of nitrogen heteroarotinoids.EBI
J Med Chem 42: 3602-14 (1999)
University Of Oklahoma Health Sciences Center
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.EBI
J Med Chem 42: 3588-601 (1999)
University Of Kansas
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.BDB
J Med Chem 42: 3572-87 (1999)
Rhone-Poulenc Rorer
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI
J Med Chem 42: 3557-71 (1999)
Rh£Ne-Poulenc Rorer
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.EBI
J Med Chem 42: 3527-38 (1999)
Southern Research Institute
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.EBI
J Med Chem 42: 3520-6 (1999)
Clinical Research Institute Of Montreal
5-deazafolate analogues with a rotationally restricted glutamate or ornithine side chain: synthesis and binding interaction with folylpolyglutamate synthetase.EBI
J Med Chem 42: 3510-9 (1999)
Harvard Medical School
CoMFA study of novel phenyl ring-substituted 3alpha-(diphenylmethoxy)tropane analogues at the dopamine transporter.EBI
J Med Chem 42: 3502-9 (1999)
National Institute On Drug Abuse-Intramural Research Program
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.EBI
J Med Chem 42: 3463-77 (1999)
Novo Nordisk
Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.EBI
J Med Chem 42: 3447-62 (1999)
Novo Nordisk
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.EBI
J Med Chem 42: 3436-46 (1999)
Georgetown University Medical Center
A multisubstrate adduct inhibitor of AICAR transformylase.EBI
J Med Chem 42: 3421-4 (1999)
The Pennsylvania State University
Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists.EBI
Bioorg Med Chem Lett 9: 2453-8 (1999)
Parke-Davis Pharmaceutical Research
Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.EBI
Bioorg Med Chem Lett 9: 2447-52 (1999)
Warner-Lambert
Synthesis of a phostone glycomimetic of the endothelin converting enzyme inhibitor phosphoramidon.EBI
Bioorg Med Chem Lett 9: 2441-6 (1999)
Université
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.EBI
Bioorg Med Chem Lett 9: 2413-8 (1999)
Cadus Pharmaceutical
Naphthazarin derivatives (II): formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity.EBI
Bioorg Med Chem Lett 9: 2407-12 (1999)
Chungnam National University
NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.EBI
Bioorg Med Chem Lett 9: 2403-6 (1999)
Abbott Laboratories
Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.EBI
Bioorg Med Chem Lett 9: 2397-402 (1999)
Fujisawa Pharmaceutical
Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors.EBI
Bioorg Med Chem Lett 9: 2391-6 (1999)
Merck Frosst Center For Therapeutic Research
Synthesis and estrogen receptor binding affinity of a porphyrin-estradiol conjugate for targeted photodynamic therapy of cancer.EBI
Bioorg Med Chem Lett 9: 2379-84 (1999)
Boston University School Of Medicine
P2-achiral, P'-extended alpha-ketoamide inhibitors of calpain I.EBI
Bioorg Med Chem Lett 9: 2371-4 (1999)
Cephalon
Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain.EBI
Bioorg Med Chem Lett 9: 2365-70 (1999)
Hoechst Marion Roussel
Structure-activity relationships of a novel class of Src SH2 inhibitors.EBI
Bioorg Med Chem Lett 9: 2359-64 (1999)
Ariad Pharmaceuticals
Structure-based design and synthesis of a novel class of Src SH2 inhibitors.EBI
Bioorg Med Chem Lett 9: 2353-8 (1999)
Ariad Pharmaceuticals
8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.EBI
Bioorg Med Chem Lett 9: 2343-8 (1999)
F. Hoffmann-La Roche
Synthesis of new (benzimidazolyl)piperazines with affinity for the 5-HT1A receptor via Pd(0) amination of bromobenzimidazoles.EBI
Bioorg Med Chem Lett 9: 2339-42 (1999)
Universidad Complutense
Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.EBI
Bioorg Med Chem Lett 9: 2335-8 (1999)
Hong Kong University Of Science And Technology
Rational herbicide design by inhibition of tryptophan biosynthesis.EBI
Bioorg Med Chem Lett 9: 2297-302 (1999)
American Cyanamid
A rapid method to identify exo-protease inhibitors.EBI
Bioorg Med Chem Lett 9: 2291-6 (1999)
The Scripps Research Institute
6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.BDB
Biochem Biophys Res Commun 262: 643-6 (1999)
Instituto De BiologÍA Celular
Structural basis for selective inhibition of Src family kinases by PP1.BDB
Chem Biol 6: 671-8 (1999)
Princeton University
Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.EBI
Bioorg Med Chem Lett 9: 2279-82 (1999)
Purdue University
Significant compensatory role of position Y-2 conferring high affinity to non-phosphorylated inhibitors of Grb2-SH2 domain.EBI
Bioorg Med Chem Lett 9: 2267-72 (1999)
National Cancer Institute-Bethesda
Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.EBI
Bioorg Med Chem Lett 9: 2259-62 (1999)
Dupont Pharmaceuticals
3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.EBI
Bioorg Med Chem Lett 9: 2233-6 (1999)
Universit£
Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).EBI
Bioorg Med Chem Lett 9: 2223-8 (1999)
Novartis Institute For Biomedical Research
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.BDB
Bioorg Med Chem Lett 9: 2217-22 (1999)
Parke-Davis Pharmaceutical Research
SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.EBI
Bioorg Med Chem Lett 9: 2207-12 (1999)
Merck Frosst Centre For Therapeutic Research
Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.EBI
Bioorg Med Chem Lett 9: 2173-6 (1999)
F. Hoffmann-La Roche
Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.EBI
Bioorg Med Chem Lett 9: 2167-72 (1999)
Uppsala University
Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers.EBI
Bioorg Med Chem Lett 9: 2151-6 (1999)
Warner-Lambert
Novel conformationally restricted tetracyclic analogs of delta8-tetrahydrocannabinol.EBI
Bioorg Med Chem Lett 9: 2119-24 (1999)
University Of Connecticut
Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.BDB
Bioorg Med Chem 7: 1281-93 (1999)
Institut Curie
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.EBI
J Med Chem 42: 3412-20 (1999)
University Of Oregon
Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.EBI
J Med Chem 42: 3356-68 (1999)
Merck Research Laboratories
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.EBI
J Med Chem 42: 3342-55 (1999)
Knoll Pharmaceuticals
Thiazolothiazepine inhibitors of HIV-1 integrase.EBI
J Med Chem 42: 3334-41 (1999)
National Cancer Institute-Bethesda
Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.EBI
J Med Chem 42: 3315-23 (1999)
University Of Kansas
Synthesis and properties of 3-(2-hydroxyethyl)-3-n-pentyldiazirine, a photoactivable general anesthetic.EBI
J Med Chem 42: 3300-7 (1999)
Massachusetts General Hospital
New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.EBI
J Med Chem 42: 3251-64 (1999)
Rh£Ne-Poulenc Rorer
Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease.EBI
J Med Chem 42: 3227-42 (1999)
Universitat De Barcelona
PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes.EBI
J Med Chem 42: 3199-202 (1999)
Wyeth-Ayerst Research
Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1-antagonists.BDB
Br J Pharmacol 127: 1288-94 (1999)
Universit&Agrove
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.BDB
Br J Pharmacol 127: 1075-82 (1999)
Roche Bioscience
Native gamma-aminobutyric acid type A receptors from rat hippocampus, containing both alpha 1 and alpha 5 subunits, exhibit a single benzodiazepine binding site with alpha 5 pharmacological properties.BDB
J Pharmacol Exp Ther 290: 989-97 (1999)
Universidad De Sevilla
Tetrapeptide derived inhibitors of complexation of a class II MHC: fully unnatural ligands.EBI
Bioorg Med Chem Lett 9: 2115-8 (1999)
Merck Research Laboratories
Tetrapeptide derived inhibitors of complexation of a class II MHC: the peptide backbone is not inviolate.EBI
Bioorg Med Chem Lett 9: 2109-14 (1999)
Merck Research Laboratories
1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.EBI
Bioorg Med Chem Lett 9: 2105-8 (1999)
Cardiff University
Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors.EBI
Bioorg Med Chem Lett 9: 2095-100 (1999)
Eisai Research Institute
Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity.EBI
Bioorg Med Chem Lett 9: 2089-94 (1999)
Merck Research Laboratories
C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study.EBI
Bioorg Med Chem Lett 9: 2085-8 (1999)
Merck Research Laboratories
Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.EBI
Bioorg Med Chem Lett 9: 2073-8 (1999)
Schering-Plough Research Institute
Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonist.EBI
Bioorg Med Chem Lett 9: 2059-64 (1999)
Centre De Recherches De Croissy
Design and synthesis of beta-carboxamido phosphonates as potent inhibitors of imidazole glycerol phosphate dehydratase.EBI
Bioorg Med Chem Lett 9: 2053-8 (1999)
Monsanto
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.EBI
Bioorg Med Chem Lett 9: 2049-52 (1999)
University Of Cambridge
Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT).EBI
Bioorg Med Chem Lett 9: 2039-42 (1999)
Azwell
Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.EBI
Bioorg Med Chem Lett 9: 2037-8 (1999)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme.EBI
Bioorg Med Chem Lett 9: 2019-24 (1999)
Warner-Lambert
Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.EBI
Bioorg Med Chem Lett 9: 2013-8 (1999)
Gorlaeus Laboratories
The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors.EBI
Bioorg Med Chem Lett 9: 1997-2002 (1999)
Southern Methodist University
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.EBI
Bioorg Med Chem Lett 9: 1991-6 (1999)
Merck Research Laboratories
The design and synthesis of inhibitors of adenosine 5'-monophosphate deaminase.EBI
Bioorg Med Chem Lett 9: 1985-90 (1999)
Agrevo
Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.EBI
Bioorg Med Chem Lett 9: 1979-84 (1999)
Fujisawa Pharmaceutical
Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2.EBI
Bioorg Med Chem Lett 9: 1973-8 (1999)
Novartis Pharmaceuticals
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.EBI
Bioorg Med Chem Lett 9: 1969-72 (1999)
UniversitäT Erlangen - NüRnberg
Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics.EBI
Bioorg Med Chem Lett 9: 1957-62 (1999)
University Of Illinois At Chicago
Isolation and structure of SCH 351633: a novel hepatitis C virus (HCV) NS3 protease inhibitor from the fungus Penicillium griseofulvum.EBI
Bioorg Med Chem Lett 9: 1949-52 (1999)
Schering-Plough Research Institute
The design and synthesis of ALS inhibitors from pharmacophore models.EBI
Bioorg Med Chem Lett 9: 1927-32 (1999)
Nankai University
Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.EBI
Bioorg Med Chem Lett 9: 1907-10 (1999)
Smithkline Beecham Pharmaceuticals
Design of benzoic acid inhibitors of influenza neuraminidase containing a cyclic substitution for the N-acetyl grouping.BDB
Bioorg Med Chem Lett 9: 1901-6 (1999)
University Of Alabama At Birmingham
Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.EBI
Bioorg Med Chem Lett 9: 1895-900 (1999)
Wyeth-Ayerst Research
Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene.EBI
J Med Chem 42: 3188-92 (1999)
University Of Bath
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.EBI
J Med Chem 42: 3154-62 (1999)
Universidad De Valencia
N(omega)-Nitroarginine-containing dipeptide amides. Potent and highly selective inhibitors of neuronal nitric oxide synthase.EBI
J Med Chem 42: 3147-53 (1999)
Northwestern University
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.EBI
J Med Chem 42: 3126-33 (1999)
University Of Georgia
Potent bivalent thrombin inhibitors: replacement of the scissile peptide bond at P(1)-P(1)' with arginyl ketomethylene isosteres.EBI
J Med Chem 42: 3109-15 (1999)
National Research Council Canada
Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships.EBI
J Med Chem 42: 3087-93 (1999)
State University Of New York
Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.EBI
J Med Chem 42: 3066-74 (1999)
Targacept
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.EBI
J Med Chem 42: 3055-65 (1999)
National Institute Of Diabetes
N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.EBI
J Med Chem 42: 3033-40 (1999)
Technische UniversitäT MüNchen
Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist.EBI
J Med Chem 42: 3026-32 (1999)
Basf
A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.EBI
J Med Chem 42: 3011-3 (1999)
TBA
Thiazole derivatives as inhibitors of purified bovine liver mitochondrial monoamine oxidase-B: structure-activity relationships and theoretical study.BDB
J Enzym Inhib 14: 307-21 (1999)
University Of Catania
Somatostatin and its receptor family.BDB
Front Neuroendocrinol 20: 157-98 (1999)
Royal Victoria Hospital
Activity-guided isolation of triterpenoid acyl CoA cholesteryl acyl transferase (ACAT) inhibitors from Ilex kudincha.EBI
J Nat Prod 62: 1061-4 (1999)
Kayaku
New guaianolides and xanthine oxidase inhibitory flavonols from ajania fruticulosaEBI
J Nat Prod 62: 1053-5 (1999)
Nanjing University
Harbinatic acid, a novel and potent DNA polymerase beta inhibitor from Hardwickia binata.EBI
J Nat Prod 62: 1000-2 (1999)
University Of Virginia
Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation.EBI
J Med Chem 42: 3004-7 (1999)
Creighton University School Of Medicine
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.EBI
J Med Chem 42: 3001-3 (1999)
Mitsui Pharmaceuticals
4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.EBI
J Med Chem 42: 2993-3000 (1999)
Cocensys
4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.EBI
J Med Chem 42: 2969-76 (1999)
Brown University
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.EBI
J Med Chem 42: 2961-8 (1999)
University Of Camerino
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.EBI
J Med Chem 42: 2909-19 (1999)
UniversitäT Hamburg
2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives.EBI
J Med Chem 42: 2870-80 (1999)
Faes
Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.EBI
J Med Chem 42: 2862-9 (1999)
University Of Minnesota
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.EBI
J Med Chem 42: 2774-97 (1999)
Universidad De Santiago
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.EBI
J Med Chem 42: 2760-73 (1999)
Dupont Pharmaceuticals
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.EBI
J Med Chem 42: 2752-9 (1999)
Dupont Pharmaceuticals
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.EBI
J Med Chem 42: 2741-6 (1999)
Novartis Institute For Biomedical Research
2-(2-Phenylcyclopropyl)imidazolines: reversed enantioselective interaction at I(1) and I(2) imidazoline receptors.EBI
J Med Chem 42: 2737-40 (1999)
Universit£
Pharmacotherapies for treatment of cocaine abuse: preclinical aspects.EBI
J Med Chem 42: 2721-36 (1999)
Research Triangle Institute
Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.BDB
Chem Biol 6: 519-29 (1999)
Institute Of Genetics And Molecular And Cellular Biology (Igbmc)
Transport of monoglucuronosyl and bisglucuronosyl bilirubin by recombinant human and rat multidrug resistance protein 2.EBI
Hepatology 30: 485-90 (1999)
Deutsches Krebsforschungszentrum
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.BDB
Acta Crystallogr D Biol Crystallogr 55: 1395-404 (1999)
Berlex
Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes.EBI
Biochem J 341: 529-35 (1999)
Physiologisch-Chemisches Institut Der Eberhard-Karls-Universit£T T£Bingen
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.EBI
J Pharmacol Exp Ther 290: 854-62 (1999)
Eli Lilly
Comparison of the pharmacological properties of cloned rat, human, and bovine norepinephrine transporters.BDB
J Pharmacol Exp Ther 290: 761-7 (1999)
The University Of Queensland
Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.BDB
J Pharmacol Exp Ther 290: 753-60 (1999)
The University Of Calgary
The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1.EBI
J Pharmacol Exp Ther 290: 672-7 (1999)
Kyorin University
Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.BDB
J Pharmacol Exp Ther 290: 551-60 (1999)
Merck Frosst Centre For Therapeutic Research
(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties.EBI
J Med Chem 42: 2716-20 (1999)
Università
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.EBI
J Med Chem 42: 2706-15 (1999)
Merck Sharp And Dohme Research Laboratories
2,7-Disubstituted amidofluorenone derivatives as inhibitors of human telomerase.EBI
J Med Chem 42: 2679-84 (1999)
The Institute Of Cancer Research
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.EBI
J Med Chem 42: 2651-61 (1999)
Schering-Plough Research Institute
Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring?EBI
J Med Chem 42: 2641-50 (1999)
Universit£
alpha-Functionalized phosphonylphosphinates: synthesis and evaluation as transcarbamoylase inhibitors.EBI
J Med Chem 42: 2633-40 (1999)
Universit£Tstrasse 16
1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists.EBI
J Med Chem 42: 2621-32 (1999)
Shionogi
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.EBI
J Med Chem 42: 2610-20 (1999)
Cea
Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives.EBI
J Med Chem 42: 2582-7 (1999)
Bial
Synthesis and serotonergic activity of substituted 2, N-benzylcarboxamido-5-(2-ethyl-1-dioxoimidazolidinyl)-N, N-dimethyltryptamine derivatives: novel antagonists for the vascular 5-HT(1B)-like receptor.EBI
J Med Chem 42: 2504-26 (1999)
Monash University (Parkville Campus)
Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.EBI
J Med Chem 42: 2498-503 (1999)
Abbott Laboratories
Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase.EBI
Bioorg Med Chem Lett 9: 1875-80 (1999)
Schering-Plough Research Institute
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.EBI
Bioorg Med Chem Lett 9: 1869-74 (1999)
Merck Research Laboratories
Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.EBI
Bioorg Med Chem Lett 9: 1831-6 (1999)
Georgetown University Medical Center
From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.EBI
Bioorg Med Chem Lett 9: 1825-30 (1999)
The James Black Foundation
Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers.EBI
Bioorg Med Chem Lett 9: 1813-8 (1999)
Warner-Lambert
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.EBI
Bioorg Med Chem Lett 9: 1807-12 (1999)
Smithkline Beecham Pharmaceuticals
Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.EBI
Bioorg Med Chem Lett 9: 1801-6 (1999)
Smithkline Beecham Pharmaceuticals
Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety.EBI
Bioorg Med Chem Lett 9: 1783-8 (1999)
Pharmacia & Upjohn
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.EBI
Bioorg Med Chem Lett 9: 1773-8 (1999)
Merck Frosst Centre For Therapeutic Research
Synthesis and identification of conformationally constrained selective MMP inhibitors.EBI
Bioorg Med Chem Lett 9: 1757-60 (1999)
Searle Discovery Research
Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors.BDB
Bioorg Med Chem Lett 9: 1751-6 (1999)
Gilead Sciences
5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.EBI
Bioorg Med Chem Lett 9: 1737-40 (1999)
Wyeth-Ayerst Research
4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.EBI
Bioorg Med Chem Lett 9: 1733-6 (1999)
Wyeth-Ayerst Research
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.EBI
Bioorg Med Chem Lett 9: 1721-6 (1999)
Georgetown University Medical Center
2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 9: 1715-20 (1999)
Merck Frosst Centre For Therapeutic Research
Synthesis and evaluation of 1-position-modified inositol 1,4,5-trisphosphate analogs.EBI
Bioorg Med Chem Lett 9: 1697-702 (1999)
The University Of Tokyo
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.EBI
Bioorg Med Chem Lett 9: 1691-6 (1999)
Universit£
Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.EBI
Bioorg Med Chem Lett 9: 1687-90 (1999)
Stanford University
Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties.EBI
Bioorg Med Chem Lett 9: 1679-82 (1999)
Universidad Complutense
Thrombin inhibitors based on [5,5] trans-fused indane lactams.EBI
Bioorg Med Chem Lett 9: 1657-62 (1999)
Glaxo Wellcome Research And Development
Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES).EBI
Bioorg Med Chem Lett 9: 1645-50 (1999)
Kingston University
A new tyrosine kinase inhibitor from the marine brown alga Stypopodium zonale.EBI
J Nat Prod 62: 927-30 (1999)
Technical University Of Braunschweig
Interference of linoleic acid fraction in some receptor binding assays.EBI
J Nat Prod 62: 912-4 (1999)
Leiden University
4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.EBI
J Med Chem 42: 2478-84 (1999)
Universita' Di Firenze
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.EBI
J Med Chem 42: 2469-77 (1999)
Cocensys
Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.EBI
J Med Chem 42: 2447-55 (1999)
Duquesne University
Structure-activity relationships for a class of inhibitors of purine nucleoside phosphorylase.EBI
J Med Chem 42: 2422-31 (1999)
University Of Michigan
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.EBI
J Med Chem 42: 2409-21 (1999)
Merck Research Laboratories
Apstatin analogue inhibitors of aminopeptidase P, a bradykinin-degrading enzyme.EBI
J Med Chem 42: 2394-402 (1999)
Pharmacia And Upjohn
Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.BDB
J Med Chem 42: 2373-82 (1999)
University Of Auckland
Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.EBI
J Med Chem 42: 2358-63 (1999)
Novartis Pharma
Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity.EBI
J Med Chem 42: 2351-7 (1999)
The University Of Wollongong
Molecular modeling and synthesis of inhibitors of herpes simplex virus type 1 uracil-DNA glycosylase.EBI
J Med Chem 42: 2344-50 (1999)
University Of Massachusetts Medical Center
Potent inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent.EBI
J Med Chem 42: 2332-43 (1999)
University Of Alabama At Birmingham
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease.BDB
Biochemistry 38: 7978-88 (1999)
University Of Queensland
Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors.EBI
Bioorg Med Chem Lett 9: 1619-24 (1999)
University Of Oregon
Design of scytalone dehydratase inhibitors as rice blast fungicides: derivatives of norephedrine.EBI
Bioorg Med Chem Lett 9: 1613-8 (1999)
Fmc Stine Research Center
Design of scytalone dehydratase inhibitors as rice blast fungicides: (N-phenoxypropyl)-carboxamides.EBI
Bioorg Med Chem Lett 9: 1607-12 (1999)
Fmc Stine Research Center
N-substituted 4-(5-indolyl)benzoic acids. Synthesis and evaluation of steroid 5alpha-reductase type I and II inhibitory activity.EBI
Bioorg Med Chem Lett 9: 1601-6 (1999)
UniversitäT Des Saarlandes
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.EBI
Bioorg Med Chem Lett 9: 1593-8 (1999)
Institute
Novel derivatives of 3-(dipropylamino)chroman. Interactions with 5-HT1A and D2A receptors.EBI
Bioorg Med Chem Lett 9: 1583-6 (1999)
Uppsala University
Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.EBI
Bioorg Med Chem Lett 9: 1573-6 (1999)
F. Hoffmann-La Roche
Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.EBI
Bioorg Med Chem Lett 9: 1553-8 (1999)
Zeria Pharmaceutical
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.EBI
Bioorg Med Chem Lett 9: 1541-6 (1999)
Eisai Research Institute
The sulfonimidamide as a novel transition state analog for aspartic acid and metallo proteases.EBI
Bioorg Med Chem Lett 9: 1527-32 (1999)
The University Of Kansas
Design of the first highly potent and selective aminopeptidase N (EC 3.4.11.2) inhibitor.EBI
Bioorg Med Chem Lett 9: 1511-6 (1999)
University Of Paris
Synthesis and evaluation of glucocerebrosidase inhibitory activity of anhydro deoxyinositols from (+)-epi- and (-)-vibo-quercitols.EBI
Bioorg Med Chem Lett 9: 1493-8 (1999)
Keio University
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.EBI
Bioorg Med Chem Lett 9: 1481-6 (1999)
Warner-Lambert
Selective substrates for non-neuronal monoamine transporters.EBI
Mol Pharmacol 56: 1-10 (1999)
University Of Heidelberg
Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.BDB
Cell Mol Neurobiol 19: 467-89 (1999)
TBA
Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.BDB
Proc Natl Acad Sci U S A 96: 7563-8 (1999)
St. Bartholomew'S And The Royal London School Of Medicine And Dentistry
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.EBI
J Med Chem 42: 2287-94 (1999)
University Of Tennessee
Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol.EBI
J Med Chem 42: 2280-6 (1999)
Laval University
Synthesis of classical and a nonclassical 2-amino-4-oxo-6-methyl-5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of thymidylate synthase.EBI
J Med Chem 42: 2272-9 (1999)
Duquesne University
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.EBI
J Med Chem 42: 2251-9 (1999)
Cea
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI
J Med Chem 42: 2235-44 (1999)
University Of GöTeborg
Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor.EBI
J Med Chem 42: 2227-34 (1999)
University Of California
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.EBI
J Med Chem 42: 2180-90 (1999)
Merck Research Laboratories
Butenolide endothelin antagonists with improved aqueous solubility.EBI
J Med Chem 42: 2162-8 (1999)
Warner-Lambert
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.EBI
J Med Chem 42: 2125-35 (1999)
Schering-Plough Research Institute
Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition.EBI
J Med Chem 42: 2112-24 (1999)
Università
A peptide agonist acts by occupation of a monomeric G protein-coupled receptor: dual sites of covalent attachment to domains near TM1 and TM7 of the same molecule make biologically significant domain-swapped dimerization unlikely.EBI
J Med Chem 42: 2105-11 (1999)
Mayo Clinic And Foundation
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.EBI
J Med Chem 42: 2087-104 (1999)
Merck Sharp & Dohme Research Laboratories
Structure-antiviral activity relationship in the series of pyrimidine and purine N-[2-(2-phosphonomethoxy)ethyl] nucleotide analogues. 1. Derivatives substituted at the carbon atoms of the base.EBI
J Med Chem 42: 2064-86 (1999)
Academy Of Sciences Of The Czech Republic
Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors.BDB
Chem Biol 6: 361-75 (1999)
University Of California Berkeley
Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.BDB
Life Sci 64: 2011-20 (1999)
Hungarian Academy Of Sciences
Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.EBI
Bioorg Med Chem Lett 9: 1469-74 (1999)
Palatin Technologies
The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.EBI
Bioorg Med Chem Lett 9: 1463-8 (1999)
Cardiff University
P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.EBI
Bioorg Med Chem Lett 9: 1453-8 (1999)
Dupont Pharmaceuticals
Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.EBI
Bioorg Med Chem Lett 9: 1447-52 (1999)
Tartu University
Uncarinic acids: phospholipase Cgamma1 inhibitors from hooks of Uncaria rhynchophylla.EBI
Bioorg Med Chem Lett 9: 1429-32 (1999)
Seoul National University
Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).EBI
Bioorg Med Chem Lett 9: 1423-8 (1999)
The R. W. Johnson Pharmaceutical Research Institute
Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.EBI
Bioorg Med Chem Lett 9: 1409-14 (1999)
Institut De Recherches Servier
Piperidine-renin inhibitors compounds with improved physicochemical properties.EBI
Bioorg Med Chem Lett 9: 1403-8 (1999)
F. Hoffmann-La Roche
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.EBI
Bioorg Med Chem Lett 9: 1397-402 (1999)
F. Hoffmann-La Roche
Efficient inhibition of muscle and liver glycogen phosphorylases by a new glucopyranosylidene-spiro-thiohydantoin.EBI
Bioorg Med Chem Lett 9: 1385-90 (1999)
Lajos Kossuth University
N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.EBI
Bioorg Med Chem Lett 9: 1379-84 (1999)
Postech
Acyl-CoA: cholesterol acyltransferase inhibitory activity of ginseng sapogenins, produced from the ginseng saponins.EBI
Bioorg Med Chem Lett 9: 1375-8 (1999)
Korea Research Institute Of Bioscience And Biotechnology
Synthesis and protein kinase C binding activity of benzolactam-V7.EBI
Bioorg Med Chem Lett 9: 1371-4 (1999)
Institute Of Organic Chemistry
S1319: a novel beta2-andrenoceptor agonist from a marine sponge Dysidea sp.EBI
Bioorg Med Chem Lett 9: 1361-4 (1999)
Kirin Brewery
trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.EBI
Bioorg Med Chem Lett 9: 1341-6 (1999)
Abbott Laboratories
Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.EBI
J Med Chem 42: 2053-9 (1999)
The Royal Danish School Of Pharmacy
Simplified pepstatins: synthesis and evaluation of N-terminally modified analogues.EBI
J Med Chem 42: 2041-5 (1999)
Institute Of Pharmaceutical Chemistry And Institute Of Pharmaceutical Technology
New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.EBI
J Med Chem 42: 2007-20 (1999)
Wyeth-Ayerst Research Laboratories
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.EBI
J Med Chem 42: 1999-2006 (1999)
Novo Nordisk
Synthesis, calcium mobilizing, and physicochemical properties of D-chiro-inositol 1,3,4,6-tetrakisphosphate, a novel and potent ligand at the D-myo-inositol 1,4,5-trisphosphate receptor.EBI
J Med Chem 42: 1991-8 (1999)
University Of Bath
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.EBI
J Med Chem 42: 1982-90 (1999)
University Of Kansas
Unique analogues of anandamide: arachidonyl ethers and carbamates and norarachidonyl carbamates and ureas.EBI
J Med Chem 42: 1975-81 (1999)
Organix
Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a.EBI
J Med Chem 42: 1965-74 (1999)
University Of Queensland
Quantitative structure-activity relationship of human neutrophil collagenase (MMP-8) inhibitors using comparative molecular field analysis and X-ray structure analysis.EBI
J Med Chem 42: 1908-20 (1999)
Hoechst Marion Roussel
Lamellarin alpha 20-sulfate, an inhibitor of HIV-1 integrase active against HIV-1 virus in cell culture.EBI
J Med Chem 42: 1901-7 (1999)
Institute Of Chemical Technology
Isoxazolo-[3,4-d]-pyridazin-7-(6H)-one as a potential substrate for new aldose reductase inhibitors.EBI
J Med Chem 42: 1894-900 (1999)
Dipartimento Di Scienze Farmaceutiche
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.EBI
J Med Chem 42: 1881-93 (1999)
Universit£
Highly potent cyclic disulfide antagonists of somatostatin.EBI
J Med Chem 42: 1863-71 (1999)
Tulane University School Of Medicine
Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R).BDB
Biochemistry 38: 7307-20 (1999)
National Institute Of Diabetes And Digestive And Kidney Diseases
Cloning and functional expression of the human histamine H3 receptor.BDB
Mol Pharmacol 55: 1101-7 (1999)
R. W. Johnson Pharmaceutical Research Institute
Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.EBI
J Med Chem 42: 1855-61 (1999)
National Institute On Aging Intramural Research Program
Synthesis and evaluation of new sulfur-containing L-arginine-derived inhibitors of nitric oxide synthase.EBI
J Med Chem 42: 1842-8 (1999)
Wake Forest University
Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.EBI
J Med Chem 42: 1803-15 (1999)
University Of Auckland
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.BDB
J Med Chem 42: 1789-802 (1999)
Japan Energy
Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.EBI
J Med Chem 42: 1757-66 (1999)
Boehringer Ingelheim Pharmaceuticals
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI
J Med Chem 42: 1749-56 (1999)
Berlex Biosciences
Homology modeling of gelatinase catalytic domains and docking simulations of novel sulfonamide inhibitors.EBI
J Med Chem 42: 1723-38 (1999)
Shionogi
4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors.EBI
J Med Chem 42: 1684-6 (1999)
Sibia Neurosciences
Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.BDB
Synapse 32: 198-211 (1999)
Mcgill University
4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.EBI
Bioorg Med Chem Lett 9: 1335-40 (1999)
Ligand Pharmaceuticals
Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.EBI
Bioorg Med Chem Lett 9: 1329-34 (1999)
Organon Laboratories
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.EBI
Bioorg Med Chem Lett 9: 1323-8 (1999)
Organon Laboratories
Optimisation of the P2 pharmacophore in a series of thrombin inhibitors: ion-dipole interactions with lysine 60G.EBI
Bioorg Med Chem Lett 9: 1317-22 (1999)
Novartis Horsham Research Center
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.EBI
Bioorg Med Chem Lett 9: 1311-6 (1999)
Merck Research Laboratories
Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.EBI
Bioorg Med Chem Lett 9: 1291-4 (1999)
Università
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.EBI
Bioorg Med Chem Lett 9: 1285-90 (1999)
Merck Sharp And Dohme Research Laboratories
Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production.EBI
Bioorg Med Chem Lett 9: 1279-84 (1999)
Dupont Pharmaceuticals
Inhibition of human telomerase by PNA-cationic peptide conjugates.EBI
Bioorg Med Chem Lett 9: 1273-8 (1999)
University Of Cambridge
Isotope edited NMR studies of glycosidases: design and synthesis of a novel glycosidase inhibitor.EBI
Bioorg Med Chem Lett 9: 1255-60 (1999)
Ohio State University
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.EBI
Bioorg Med Chem Lett 9: 1251-4 (1999)
Merck Research Laboratories
Synthesis and evaluation of geldanamycin-estradiol hybrids.EBI
Bioorg Med Chem Lett 9: 1233-8 (1999)
Sloan-Kettering Institute For Cancer Research
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.EBI
Bioorg Med Chem Lett 9: 1227-32 (1999)
Research And Development
Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506.EBI
Bioorg Med Chem Lett 9: 1219-24 (1999)
Banyu Tsukuba Research Institute
Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.BDB
J Pharmacol Exp Ther 289: 1262-70 (1999)
Banyu Pharmaceutical
Pharmacological characterization of nicotine's interaction with cocaine and cocaine analogs.BDB
J Pharmacol Exp Ther 289: 1229-36 (1999)
Virginia Commonwealth University
Synthesis of the quinoline-linked triazolopyrimidine analogues and their interactions with the recombinant tobacco acetolactate synthase.EBI
Biochem Biophys Res Commun 258: 797-801 (1999)
Seoul Women'S University
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.EBI
Bioorg Med Chem Lett 9: 1195-200 (1999)
Dupont Pharmaceuticals
Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.EBI
Bioorg Med Chem Lett 9: 1185-8 (1999)
Dupont Pharmaceuticals
Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases.EBI
Bioorg Med Chem Lett 9: 1179-84 (1999)
Biomolecular Engineering Research Institute
Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 9: 1171-4 (1999)
G.D. Searle-Monsanto
Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors.EBI
Bioorg Med Chem Lett 9: 1167-70 (1999)
G.D. Searle-Monsanto
Synthesis and biological activity of trans-2,3-dihydroraloxifene.EBI
Bioorg Med Chem Lett 9: 1137-40 (1999)
Eli Lilly
Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.EBI
Bioorg Med Chem Lett 9: 1121-6 (1999)
Warner-Lambert
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.EBI
Bioorg Med Chem Lett 9: 1103-8 (1999)
Novartis Horsham Research Centre
Synthesis of caged peptides using caged lysine: application to the synthesis of caged AIP, a highly specific inhibitor of calmodulin-dependent protein kinase II.EBI
Bioorg Med Chem Lett 9: 1093-6 (1999)
Osaka National Research Institute
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.EBI
Bioorg Med Chem Lett 9: 1069-74 (1999)
Abbott Laboratories
Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.BDB
Neuropsychopharmacology 20: 612-27 (1999)
University Of North Carolina
Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.BDB
Chem Biol 6: 265-75 (1999)
Ligand Pharmaceuticals
Structure-based discovery and in-parallel optimization of novel competitive inhibitors of thymidylate synthase.BDB
Chem Biol 6: 319-31 (1999)
Northwestern University
Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.EBI
Bioorg Med Chem Lett 9: 1063-6 (1999)
Dupont Pharmaceuticals
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.EBI
Bioorg Med Chem Lett 9: 1057-62 (1999)
Dupont Pharmaceuticals
Thrombin inhibitors based on a propargylglycine template.EBI
Bioorg Med Chem Lett 9: 1013-8 (1999)
Biotech Research Institute
Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.EBI
Bioorg Med Chem Lett 9: 1009-12 (1999)
Ligand Pharmaceuticals
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.EBI
Bioorg Med Chem Lett 9: 1003-8 (1999)
Ligand Pharmaceuticals
6-(1-Hydroxyalkyl))penam sulfone derivatives as inhibitors of class A and class C beta-lactamases II.EBI
Bioorg Med Chem Lett 9: 997-1002 (1999)
Wyeth-Ayerst Research
6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C beta-lactamases I.EBI
Bioorg Med Chem Lett 9: 991-6 (1999)
Wyeth-Ayerst Research
N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.EBI
Bioorg Med Chem Lett 9: 979-84 (1999)
The R. W. Johnson Pharmaceutical Research Institute
Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against acetylcholinesterase: unique structural analogs of tacrine based on the BCD-ring of arisugacin.EBI
Bioorg Med Chem Lett 9: 973-8 (1999)
University Of Minnesota
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.EBI
Bioorg Med Chem Lett 9: 967-72 (1999)
Dupont Pharmaceuticals
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.EBI
Bioorg Med Chem Lett 9: 943-8 (1999)
Searle Discovery Research
Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.EBI
Bioorg Med Chem Lett 9: 937-42 (1999)
Dupont Pharmaceuticals
Adenosine receptor ligands with oxygenated N6-substituents.EBI
Bioorg Med Chem Lett 9: 933-6 (1999)
Deakin University
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.EBI
Bioorg Med Chem Lett 9: 925-30 (1999)
Dupont Pharmaceuticals
Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.EBI
Bioorg Med Chem Lett 9: 919-24 (1999)
Dupont Pharmaceuticals
Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.EBI
Bioorg Med Chem Lett 9: 913-8 (1999)
Biochem Therapeutic
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.EBI
J Med Chem 42: 1673-9 (1999)
National Institute Of Diabetes
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.EBI
J Med Chem 42: 1648-60 (1999)
Pierre Fabre Research Center
Cyclobutane quisqualic acid analogues as selective mGluR5a metabotropic glutamic acid receptor ligands.EBI
J Med Chem 42: 1639-47 (1999)
University Of Minnesota
Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.EBI
J Med Chem 42: 1625-38 (1999)
National Institute Of Diabetes
Development of fluorine-18-labeled 5-HT1A antagonists.EBI
J Med Chem 42: 1576-86 (1999)
National Institutes Of Health
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.EBI
J Med Chem 42: 1556-75 (1999)
Universit£
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.EBI
J Med Chem 42: 1546-55 (1999)
Parc Club Orsay Université
Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.EBI
J Med Chem 42: 1537-45 (1999)
University Of Alabama At Birmingham
Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors.EBI
J Med Chem 42: 1525-36 (1999)
Pharmacia And Upjohn
Potent estrogenic agonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore.EBI
J Med Chem 42: 1501-4 (1999)
University Of Tokyo
Emerging molecular approaches to pain therapy.EBI
J Med Chem 42: 1481-500 (1999)
Abbott Laboratories
Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.BDB
Schizophr Res 37: 107-22 (1999)
Eli Lilly
Structural elements of the gamma-aminobutyric acid type A receptor conferring subtype selectivity for benzodiazepine site ligands.BDB
J Biol Chem 274: 13370-4 (1999)
SynthÉLabo
A transfected cell model for the renal toxin transporter, rOCT2.EBI
Toxicol Sci 47: 181-6 (1999)
University Of Texas M. D. Anderson Cancer Center
Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.EBI
Mol Pharmacol 55: 847-54 (1999)
Kyorin University
Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis.BDB
Bioorg Med Chem 7: 351-7 (1999)
Hong Kong University Of Science And Technology
Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.BDB
J Pharmacol Exp Ther 289: 1151-9 (1999)
Gliatech
Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001.BDB
J Pharmacol Exp Ther 289: 926-35 (1999)
Taisho Pharmaceutical
5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.EBI
J Med Chem 42: 1466-72 (1999)
Ligand Pharmaceuticals
Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.EBI
J Med Chem 42: 1428-40 (1999)
University Of California
Chicoric acid analogues as HIV-1 integrase inhibitors.EBI
J Med Chem 42: 1401-14 (1999)
National Cancer Institute-Bethesda
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.EBI
J Med Chem 42: 1393-400 (1999)
Leiden/Amsterdam Center For Drug Research
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.EBI
J Med Chem 42: 1384-92 (1999)
Leiden University
Bound structures of novel P3-P1' beta-strand mimetic inhibitors of thrombin.EBI
J Med Chem 42: 1376-83 (1999)
Michigan State University
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI
J Med Chem 42: 1367-75 (1999)
Molecumetics
Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines.EBI
J Med Chem 42: 1348-57 (1999)
Affymax Research Institute
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.EBI
J Med Chem 42: 1333-40 (1999)
Yale University
N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.EBI
Bioorg Med Chem Lett 9: 907-12 (1999)
Warner-Lambert
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.EBI
Bioorg Med Chem Lett 9: 901-6 (1999)
Schering-Plough Research Institute
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.EBI
Bioorg Med Chem Lett 9: 895-900 (1999)
Corvas International
Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.EBI
Bioorg Med Chem Lett 9: 875-80 (1999)
Sankyo
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.EBI
Bioorg Med Chem Lett 9: 863-8 (1999)
Merck Research Laboratories
Bicyclo[3.2.1]octanes: synthesis and inhibition of binding at the dopamine and serotonin transporters.EBI
Bioorg Med Chem Lett 9: 857-62 (1999)
Organix
Synthesis and activity of gamma-(L-gamma-azaglutamyl)-S-(p-bromobenzyl)-L-cysteinylglycine: a metabolically stable inhibitor of glyoxalase I.EBI
Bioorg Med Chem Lett 9: 853-6 (1999)
University Of Minnesota
Novel reverse-turn mimics inhibit farnesyl transferase.EBI
Bioorg Med Chem Lett 9: 847-52 (1999)
Cold Spring Harbor Laboratory
Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.EBI
Bioorg Med Chem Lett 9: 841-6 (1999)
Universit£T Erlangen-N£Rnberg
Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.EBI
Bioorg Med Chem Lett 9: 835-40 (1999)
Warner-Lambert
Ring constrained analogues of the orvinols: the furanomorphides.EBI
Bioorg Med Chem Lett 9: 831-4 (1999)
University Of Bristol
Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.EBI
Bioorg Med Chem Lett 9: 815-20 (1999)
Warner-Lambert
A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor.EBI
Bioorg Med Chem Lett 9: 803-6 (1999)
Kyoto Pharmaceutical University
Synthesis of alpha-C(1-->3)-mannopyranoside of N-acetylgalactosamine, a new beta-galactosidase inhibitor.EBI
Bioorg Med Chem Lett 9: 793-6 (1999)
Institut De Chimie Organique De L'Université
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.EBI
Bioorg Med Chem Lett 9: 775-80 (1999)
Eli Lilly
Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.EBI
Bioorg Med Chem Lett 9: 765-70 (1999)
Agouron Pharmaceuticals
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.EBI
Bioorg Med Chem Lett 9: 755-8 (1999)
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.EBI
Bioorg Med Chem Lett 9: 749-54 (1999)
Merck Research Laboratories
A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids.EBI
Bioorg Med Chem Lett 9: 743-8 (1999)
Allergan
Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.EBI
Bioorg Med Chem Lett 9: 737-42 (1999)
Novartis Horsham Research Center
Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.EBI
Bioorg Med Chem Lett 9: 703-8 (1999)
Abbott Laboratories
First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines.EBI
Bioorg Med Chem Lett 9: 691-6 (1999)
Pohang University Of Science And Technology
1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.EBI
Bioorg Med Chem Lett 9: 685-90 (1999)
Nv Organon
Synthesis and activity of 2-(sulfonamido)methyl-carbapenems: discovery of a novel, anti-MRSA 1,8-naphthosultam pharmacophore.EBI
Bioorg Med Chem Lett 9: 673-8 (1999)
Merck Research Laboratories
Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.EBI
Bioorg Med Chem Lett 9: 667-72 (1999)
Albert Szent-Gy£Rgyi Medical University
Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.EBI
Bioorg Med Chem Lett 9: 663-6 (1999)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.EBI
Bioorg Med Chem Lett 9: 647-52 (1999)
Eli Lilly
Potent, orally absorbed glucagon receptor antagonists.EBI
Bioorg Med Chem Lett 9: 641-6 (1999)
Merck Research Laboratories
PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.EBI
Biochem Biophys Res Commun 257: 410-3 (1999)
University Of Tennessee Medical Center
Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.EBI
J Med Chem 42: 1312-9 (1999)
University Of Montpellier
Quinuclidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase: optimization from lipid profiles.EBI
J Med Chem 42: 1306-11 (1999)
Zeneca Pharmaceuticals
1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.EBI
J Med Chem 42: 1293-305 (1999)
Tanabe Seiyaku
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.EBI
J Med Chem 42: 1274-81 (1999)
Merck Frosst Centre For Therapeutic Research
Enzyme-assisted total synthesis of the optical antipodes D-myo-inositol 3,4,5-trisphosphate and D-myo-inositol 1,5, 6-trisphosphate: aspects of their structure-activity relationship to biologically active inositol phosphates.EBI
J Med Chem 42: 1262-73 (1999)
Bergische UniversitäT Wuppertal
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.EBI
J Med Chem 42: 1235-49 (1999)
Boehringer Ingelheim Pharma
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements.EBI
J Med Chem 42: 1213-24 (1999)
Agouron Pharmaceuticals
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics.EBI
J Med Chem 42: 1203-12 (1999)
Agouron Pharmaceuticals
Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.EBI
J Med Chem 42: 1193-202 (1999)
University Of Kuopio
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.EBI
J Med Chem 42: 1178-92 (1999)
Dupont Pharmaceuticals
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series.EBI
J Med Chem 42: 1161-9 (1999)
Warner-Lambert
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series.EBI
J Med Chem 42: 1151-60 (1999)
Warner-Lambert
Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.EBI
J Med Chem 42: 1115-22 (1999)
Vrije Universiteit
Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter.EBI
Nat Neurosci 1: 349-51 (1999)
University Of Heidelberg
ATP- and glutathione-dependent transport of chemotherapeutic drugs by the multidrug resistance protein MRP1.EBI
Br J Pharmacol 126: 681-8 (1999)
University Hospital Groningen
Solid-phase synthesis of novel inhibitors of farnesyl transferase.EBI
Bioorg Med Chem Lett 9: 623-6 (1999)
Institute Of Cancer Research
Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.EBI
Bioorg Med Chem Lett 9: 619-22 (1999)
Merck
Homoisofagomines: chemical-enzymatic synthesis and evaluation as alpha- and beta-glucosidase inhibitors.EBI
Bioorg Med Chem Lett 9: 615-8 (1999)
Technische Universit£T Berlin
Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.EBI
Bioorg Med Chem Lett 9: 589-94 (1999)
Allergan
Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.EBI
Bioorg Med Chem Lett 9: 585-8 (1999)
Merck Sharp & Dohme Research Laboratories
High affinity retinoic acid receptor antagonists: analogs of AGN 193109.EBI
Bioorg Med Chem Lett 9: 573-6 (1999)
Allergan
Nonpeptide small-molecular inhibitors of dipeptidyl peptidase IV: N-phenylphthalimide analogs.EBI
Bioorg Med Chem Lett 9: 559-62 (1999)
University Of Tokyo
Inhibition of 4-hydroxyphenylpyruvate dioxygenase by sethoxydim, a potent inhibitor of acetyl-coenzyme A carboxylase.EBI
Bioorg Med Chem Lett 9: 551-4 (1999)
Tunghai Christian University
Synthesis of 5,8-dimethoxy-3-hydroxy-4-quinolone, a reported inhibitor of HIV RT, and evidence the original proposed structure was incorrect.EBI
Bioorg Med Chem Lett 9: 543-6 (1999)
Medichem Research
(3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.EBI
Bioorg Med Chem Lett 9: 533-8 (1999)
Kyorin Pharmaceutical
Synthesis and biological evaluation of alpha,alpha-difluorobenzylphosphonic acid derivatives as small molecular inhibitors of protein-tyrosine phosphatase 1B.EBI
Bioorg Med Chem Lett 9: 529-32 (1999)
Tokyo University Of Pharmacy & Life Science
Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene.EBI
Bioorg Med Chem Lett 9: 523-8 (1999)
Eli Lilly
bis-5-Alkylresorcinols from Panopsis rubescens that inhibit DNA polymerase beta.EBI
J Nat Prod 62: 477-80 (1999)
University Of Virginia
New phenolic and quinone-methide triterpenes from Maytenus amazonica.EBI
J Nat Prod 62: 434-6 (1999)
Universidad De La Laguna
Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.EBI
Bioorg Med Chem Lett 9: 491-6 (1999)
Merck Research Laboratories
2D