PMID

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Article Title

Organization

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University of Florida

Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.

Berlex Biosciences

Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.

Lg Life Sciences

GRID/CPCA: a new computational tool to design selective ligands.

Boehringer Ingelheim Pharma

Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.

R. W. Johnson Pharmaceutical Research Institute

Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.

University of Arkansas

New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue.

Cnrs-Cercoa

Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.

Abbott Laboratories

Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.

Medical University of South Carolina

 

Peptidyl -keto thiazole as potent thrombin inhibitors

TBA

 

Design and synthesis of conformationally constrained arginal thrombin inhibitors

TBA

 

Rational design of selective thrombin inhibitors

TBA

 

Synthesis and biological activity of P₂–P₄ azapeptidomimetic P₁-argininal and P₁-ketoargininamide derivatives: a novel class of serine protease inhibitors

TBA

 

Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor

TBA

 

Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif

TBA

 

Characterization of LY806303 as a potent and selective inhibitor of thrombin

TBA

Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.

University of Antwerp

Inhibition of trypsin and urokinase by Cbz-amino(4-guanidinophenyl)methanephosphonate aromatic ester derivatives: the influence of the ester group on their biological activity.

Wroclaw University of Technology

Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.

Boehringer Ingelheim Pharma

Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Shionogi

Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.

Lg Chemical

Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.

Shionogi

Isoxazolines and isoxazoles as factor Xa inhibitors.

Dupont Pharmaceuticals

Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.

Berlex Biosciences

Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.

3-Dimensional Pharmaceuticals

Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.

3-Dimensional Pharmaceuticals

3-Amidinophenylalanine-based inhibitors of urokinase.

UniversitäT Jena

Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.

Biotech Research Institute

Thrombin inhibitors based on a propargylglycine template.

Biotech Research Institute

Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.

Nv Organon Scientific Development Group

Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.

Institut FüR Biochemie

Benzylamine-based selective and orally bioavailable inhibitors of thrombin.

Biotech Research Institute

Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.

Berlex Biosciences

Potent and efficacious thienylamidine-incorporated thrombin inhibitors.

Biotech Research Institute

Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.

Novartis Pharma

(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.

Berlex Biosciences

2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.

Warner-Lambert

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.

Merck Research Laboratories

Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.

Thrombosis Research Institute

Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.

Eli Lilly

Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.

TBA

Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.

Merck Sharp and Dohme Research Laboratories

Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.

University of Illinois

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.

Centre De Recherches De Croissy

OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.

Second Tokushima Institute of New Drug Research

Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.

F. Hoffmann-La Roche

Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.

University of California Berkeley

Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.

University of California San Francisco

Chemical phylogenetics of histone deacetylases.

Dana-Farber Cancer Institute

Inhibition of a viral enzyme by a small-molecule dimer disruptor.

University of California San Francisco

Diastereomeric molecular recognition and binding behavior of bile acids by L/D-tryptophan-modified beta-cyclodextrins.

Nankai University

 

A Thermodynamic Study of the Reactions of Cyclodextrins with Primary and Secondary Aliphatic Alcohols, with D- and L-Phenylalanine, and with L-Phenylalanine Amide

Nist

Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts.

Universitat De Barcelona

HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.

Rutgers University

Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.

University of Athens