457 articles for thisTarget
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Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate.
China Pharmaceutical University
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.
Ecole Polytechnique F�D�Rale De Lausanne Epfl
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.
Bristol-Myers Squibb R & D
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.
University Of Ljubljana
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
On scaffold hopping: challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans.
Virginia Commonwealth University
Statistical molecular design, parallel synthesis, and biological evaluation of a library of thrombin inhibitors.
Astrazeneca
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Celera Genomics
Development of activity-based probes for trypsin-family serine proteases.
Celera Genomics
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.
Berlex Biosciences
Argatroban analogs: Synthesis, thrombin inhibitory activity and cell permeability of aminoheterocyclic guanidine surrogates
TBA
Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis.
University Of Ljubljana
Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2).
Caprotec Bioanalytics
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
Aarhus University
Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.
Virginia Commonwealth University
Active site mapping of trypsin, thrombin and matriptase-2 by sulfamoyl benzamidines.
University Of Bonn
Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.
Zydus Research Centre
Ligand binding stepwise disrupts water network in thrombin: enthalpic and entropic changes reveal classical hydrophobic effect.
Philipps University Marburg
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.
Hokkaido University
Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity.
China Pharmaceutical University
Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.
Astrazeneca
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.
Virginia Commonwealth University
A new strategy for the development of highly potent and selective plasmin inhibitors.
Philipps University Marburg
Photoregulation of thrombin aptamer activity using Bhc caging strategy.
University Of Science And Technology Of China
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.
Takeda Pharmaceutical
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University Of Florida
Cyclotheonamides E2 and E3, new potent serine protease inhibitors from the marine sponge of the genus Theonella.
The University Of Tokyo
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Johnson & Johnson Pharmaceutical Research & Development
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.
Takeda Pharmaceutical
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.
Takeda Pharmaceutical
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.
Merck Research Laboratories
Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs.
Universit£
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bristol-Myers Squibb Research And Development
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.
University Of Antwerp
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
Bristol-Myers Squibb
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.
Daiichi Asubio Medical Research Laboratories
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Pfizer
Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.
Universit£
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.
Brown University
Conformation mining: an algorithm for finding biologically relevant conformations.
Rational Discovery
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities.
University Of Ljubljana
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.
Central Pharmaceutical Research Institute
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
Berlex Biosciences
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Merck Research Laboratories
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.
Central Pharmaceutical Research Institute
Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.
Central Pharmaceutical Research Institute
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
Merck Research Laboratories
Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives.
Link£Ping University
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
Pharmaceutical Research Institute
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.
Pharmacia
Synthesis and SAR of thrombin inhibitors incorporating a novel 4-amino-morpholinone sscaffold: analysis of X-ray crystal structure of enzyme inhibitor complex.
Link£Ping University
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
Thrombin inhibition by novel benzamidine derivatives: a free-energy perturbation study.
Universidade Federal Do Rio De Janeiro
Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.
Research And Development
Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.
Berlex Biosciences
Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.
University Of Parma
Estimation of binding affinities for selective thrombin inhibitors via Monte Carlo simulations.
Yale University
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Dupont Pharmaceuticals
Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.
Universit£
New proline mimetics: synthesis of thrombin inhibitors incorporating cyclopentane- and cyclopentenedicarboxylic acid templates in the P2 position. Binding conformation investigated by X-ray crystallography.
Link£Ping University
GRID/CPCA: a new computational tool to design selective ligands.
Boehringer Ingelheim Pharma
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.
Novartis Horsham Research Centre
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Rh£Ne-Poulenc Rorer
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.
Rh£Ne-Poulenc Rorer
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.
Dupont Pharmaceuticals
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
Merck Research Laboratories
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.
3-Dimensional Pharmaceuticals
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.
Merck Research Laboratories
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Merck Research Laboratories
Synthesis and pharmacological properties of a close analogue of an antithrombotic pentasaccharide (SR 90107A/ORG 31540).
Sanofi Recherche
Binding affinities for sulfonamide inhibitors with human thrombin using Monte Carlo simulations with a linear response method.
Yale University
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
Design and synthesis of potent and highly selective thrombin inhibitors.
F. Hoffmann-La Roche
Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.
Thrombosis Research Institute
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Maxim Pharmaceuticals
Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.
3-Dimensional Pharmaceuticals
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Merck Research Laboratories
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.
Pharmacia
D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.
Basf
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.
Life Science R & D, Lgci
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.
Corvas International
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.
Universit£
Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.
Bristol-Myers Squibb Pharmaceutical Research Institute
Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.
Bristol-Myers Squibb Pharmaceutical Research Institute
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.
Medical University Of South Carolina
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.
Dupont Pharmaceuticals
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.
Universit£
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.
Novartis Horsham Research Centre
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.
Research And Development
1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.
Nv Organon
Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.
Nv Organon
Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.
Rh£Ne-Poulenc Rorer
Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.
Gorlaeus Laboratories
Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics.
University Of Illinois At Chicago
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).
Institute For Drug Research
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.
University Of Ljubljana
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).
University Of Antwerp
Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.
Sanofi Pharmaceuticals
Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases.
University Of Heidelberg
Conformationally restricted analogs of the direct thrombin inhibitor FM 19.
University Of Michigan
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.
Universit£T Bielefeld
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.
Astellas Pharma
HLE-inhibitory alkaloids with a polyketide skeleton from the marine-derived fungus Coniothyrium cereale.
University Of Bonn
Synthesis and biochemical evaluation of triazole/tetrazole-containing sulfonamides against thrombin and related serine proteases.
The Johns Hopkins University
Thermodynamic and biological evaluation of a thrombin binding aptamer modified with several unlocked nucleic acid (UNA) monomers and a 2'-C-piperazino-UNA monomer.
University Of Southern Denmark
Rational design of potent, small, synthetic allosteric inhibitors of thrombin.
Virginia Commonwealth University
Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities.
University Of Ljubljana
Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.
Universit£
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.
Philipps University Marburg
Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.
Technical University Of Denmark
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.
Merck Research Laboratories
P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.
Merck Research Laboratories
New furin inhibitors based on weakly basic amidinohydrazones.
Philipps University Marburg
Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.
Université
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
F. Hoffmann-La Roche
Identification of the first low-molecular-weight inhibitors of matriptase-2.
University Of Bonn
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.
University Of Basel
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.
Takeda Pharmaceutical
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
Johnson & Johnson Pharmaceutical Research And Development
Micropeptins from an Israeli fishpond water bloom of the cyanobacterium Microcystis sp.
Tel-Aviv University
Enhancement of hydrophobic interactions and hydrogen bond strength by cooperativity: synthesis, modeling, and molecular dynamics simulations of a congeneric series of thrombin inhibitors.
The State University Of New York
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Philipps University Marburg
From natural products to achiral drug prototypes: potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs.
Universit£
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Bristol-Myers Squibb
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.
F. Hoffmann-La Roche
Preparation of L-proline based aeruginosin 298-A analogs: optimization of the P1-moiety.
University Of New Orleans
Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor.
University Of Montpellier
Peptide argininol “inverse substrates” of anisic acid: Novel inhibitors of the trypsin-like serine proteinases
TBA
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety
TBA
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors
TBA
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogates
TBA
An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatran
TBA
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates
TBA
RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLES
TBA
Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor
TBA
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors
TBA
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.
Millennium Pharmaceuticals
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Millennium Pharmaceuticals
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.
The Medicines Company (Leipzig)
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.
Daiichi Sankyo
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.
Curacyte Discovery
3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.
University Of Ljubljana
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.
Chugai Pharmaceutical
Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.
Kissei Pharmaceutical
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Bristol-Myers Squibb
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.
Takeda Pharmaceutical
Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.
University Of Ljubljana
Structure of a novel thrombin inhibitor with an uncharged D-amino acid as P1 residue.
Institut FüR Biochemie
Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.
Griffith University
Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge.
Kirin Brewery
Isolation of translactone-containing triterpenes with thrombin inhibitory activities from the leaves of Lantana camara.
Glaxo Wellcome Research And Development
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.
Chinese Academy Of Sciences
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.
Pfizer
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.
Daiichi Pharmaceutical
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.
Curacyte Discovery
Structure-based organic synthesis of unnatural aeruginosin hybrids as potent inhibitors of thrombin.
Université
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Glaxosmithkline
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.
Astellas Pharma
Sulfonamide-related conformational effects and their importance in structure-based design.
Glaxosmithkline
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.
Astellas Pharma
Synthesis and evaluation of a small library of graftable thrombin inhibitors derived from (L)-arginine.
Université
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.
University Of Antwerp
Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.
Institut De Recherches Servier
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Celera Genomics
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
Celera
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.
Mochida Pharmaceutical
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.
Johnson & Johnson Pharmaceutical Research And Development
Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.
University Of Namur
3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa.
University Of Namur
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Celera
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles.
Merck Research Laboratories
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.
National Research Council Of Canada
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.
Merck Research Laboratories
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.
Daiichi Pharmaceutical
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Eli Lilly
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Merck Research Laboratories
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.
Aventis Pharma Deutschland
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.
University Of Ljubljana
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Abbott Laboratories
A novel series of potent and selective small molecule inhibitors of the complement component C1s.
3-Dimensional Pharmaceuticals
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.
Daiichi Pharmaceutical
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.
University Of Antwerp
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.
The Bristol-Myers Squibb Pharmaceutical Research Institute
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.
Millennium Pharmaceuticals
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
Millennium Pharmaceuticals
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.
Millennium Pharmaceuticals
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Millennium Pharmaceuticals
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.
Millennium Pharmaceuticals
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.
Johnson & Johnson Pharmaceutical Research & Development
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
Abbott Laboratories
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.
Pharmacia
Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.
Glaxosmithkline
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.
Merck Research Laboratories
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.
University Of Ljubljana
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
Pharmacia
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.
Boehringer Ingelheim Pharma
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.
Boehringer Ingelheim Pharma
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.
Ajinomoto
Generation of ligand conformations in continuum solvent consistent with protein active site topology: application to thrombin.
Thrombosis Research Institute
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.
3-Dimensional Pharmaceuticals
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.
Aventis Pharma Deutschland
High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition.
Molecumetics
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.
Merck Research Laboratories
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Merck Research Laboratories
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.
Millennium Pharmaceuticals
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.
Millennium Pharmaceuticals
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.
Merck Research Laboratories
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.
University Of Ljubljana
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.
Senju Pharmaceutical
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.
Aventis Pharmaceuticals
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Merck Research Laboratories
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.
Millennium Pharmaceuticals
Design and synthesis of factor Xa inhibitors and their prodrugs.
Millennium Pharmaceuticals
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Merck Research Laboratories
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.
Millennium Pharmaceuticals
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
Celera
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
Celera
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Aventis Pharmaceuticals
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.
Aventis Pharmaceuticals
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.
Millennium Pharmaceuticals
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.
Millennium Pharmaceuticals
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.
Millennium Pharmaceuticals
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.
Berlex Biosciences
Structure-based design of novel potent nonpeptide thrombin inhibitors.
Boehringer Ingelheim Pharma
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.
Aventis Pharmaceuticals
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.
Corvas International
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.
Protherics Molecular Design
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).
Merck Research Laboratories
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxohexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 2. Potency and chirality.
Glaxosmithkline
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.
Axys Pharmaceuticals
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.
Cor Therapeutics
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.
Cor Therapeutics
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.
Axys Pharmaceuticals
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.
Axys Pharmaceuticals
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.
3-Dimensional Pharmaceuticals
Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.
Georgetown University Medical Center
Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.
The R. W. Johnson Pharmaceutical Research Institute
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.
Prosthetics Molecular Design
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.
Dupont Pharmaceuticals
Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.
Biochem Pharma
Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.
Aventis Pharma
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 1. The alpha-methyl-trans-lactam template.
Glaxo Wellcome Research And Development
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.
Dupont Pharmaceuticals
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Shionogi
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
Shionogi
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.
Pfizer
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.
Axys Pharmaceuticals
Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.
Axys Pharmaceuticals
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.
Corvas International
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.
Novartis Horsham Research Centre
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.
Dupont Pharmaceuticals
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.
Berlex Biosciences
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.
Berlex Biosciences
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.
Merck Research Laboratories
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.
Corvas International
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.
Rhone-Poulenc Rorer
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.
Warner-Lambert
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
Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor.
3-Dimensional Pharmaceuticals
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.
Cor Therapeutics
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
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.
Corvas International
Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.
Yoshitomi Pharmaceutical Industries
Two-stage method for protein-ligand docking.
German National Research Center For Information Technology
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.
RhôNe-Poulenc Rorer
Asymmetric synthesis of novel quaternary alpha-hydroxy-delta-lactam dipeptide surrogates.
Corvas International
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.
Warner-Lambert
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.
Warner-Lambert
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
Biotech Research Institute
Potent bivalent thrombin inhibitors: replacement of the scissile peptide bond at P(1)-P(1)' with arginyl ketomethylene isosteres.
National Research Council Canada
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.
Dupont Pharmaceuticals
Thrombin inhibitors based on [5,5] trans-fused indane lactams.
Glaxo Wellcome Research And Development
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.
Berlex Biosciences
Optimisation of the P2 pharmacophore in a series of thrombin inhibitors: ion-dipole interactions with lysine 60G.
Novartis Horsham Research Center
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.
Novartis Horsham Research Centre
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.
Dupont Pharmaceuticals
Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.
Biochem Therapeutic
Bound structures of novel P3-P1' beta-strand mimetic inhibitors of thrombin.
Michigan State University
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.
Molecumetics
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.
Corvas International
Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.
Warner-Lambert
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.
Eli Lilly
Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.
Novartis Horsham Research Center
Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin.
Glaxo Wellcome Research And Development
Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.
Nv Organon Scientific Development Group
The discovery of orally available thrombin inhibitors: studies towards the optimisation of CGH1668.
Novartis Horsham Research Center
Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.
Warner-Lambert
Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications.
Biochem Therapeutic
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.
Glaxo Wellcome Research And Development
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.
Dupont Pharmaceuticals
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
Biotech Research Institute
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.
Corvas International
Templates for design of inhibitors for serine proteases: application of the program DOCK to the discovery of novel inhibitors for thrombin.
Wayne State University
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.
Molecumetics
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.
Berlex Biosciences
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
Merck Research Laboratories
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.
Merck Research Laboratories
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.
Biotech Research Institute
Identification of a potent analogue of Nazumamide A through iteration of combinatorial tetrapeptide libraries.
Central Drug Research Institute
Diarylsulfonamides as selective, non-peptidic thrombin inhibitors.
Pharmazeutisch-Chemisches Institut Der UniversitäT
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.
3-Dimensional Pharmaceuticals
1,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors.
Menarini Ricerche
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.
Dupont Pharmaceuticals
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
Biotech Research Institute
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Merck Research Laboratories
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.
Dupont Pharmaceuticals
Solid phase synthesis of benzylamine-derived sulfonamide library.
Biotech Research Institute
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.
Bristol-Myers Squibb Pharmaceutical Research Institute
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.
Merck Research Laboratories
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
Glaxowellcome Medicines Research Centre
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.
Novartis Pharma
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
Berlex Biosciences
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.
Berlex Biosciences
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Merck Research Laboratories
Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.
Merck Research Laboratories
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.
Collegeville
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.
Dupont Pharmaceuticals
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Merck Research Laboratories
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.
RhôNe-Poulenc Rorer
Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.
Chinese Academy Of Sciences
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.
Merck Research Laboratories
Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.
Corvas International
Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.
Corvas International
The solution conformation of (D)Phe-Pro-containing peptides: implications on the activity of Ac-(D)Phe-Pro-boroArg-OH, a potent thrombin inhibitor.
Dupont Pharmaceuticals
Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series.
Bristol-Myers Squibb Pharmaceutical Research Institute
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.
Daiichi Pharmaceutical
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.
Bristol-Myers Squibb Pharmaceutical Research Institute
Binding of fluorescent and spin-labeled C-terminal hirudin analogs to thrombin.
Ohio State University
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.
Thrombosis Research Institute
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.
Zeneca Pharmaceuticals
Synthesis of a homologous series of ketomethylene arginyl pseudodipeptides and application to low molecular weight hirudin-like thrombin inhibitors.
National Research Council Of Canada
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
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
University Of California San Francisco
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.
Merck Research Laboratories
Ethylene biosynthesis: processing of a substrate analog supports a radical mechanism for the ethylene-forming enzyme.
Duke University
Engineering novel specificities for ligand-activated transcription in the nuclear hormone receptor RXR.
University Of Texas Southwestern Medical Center
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.
Smithkline Beecham Pharmaceuticals
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.
University Of California San Diego
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.
University Of California Berkeley
Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis.
Cgi Pharmaceuticals
Ultrasensitive in situ visualization of active glucocerebrosidase molecules.
Leiden University
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Novartis Institutes For Biomedical Research
Picomolar inhibitors as transition-state probes of 5'-methylthioadenosine nucleosidases.
Albert Einstein College Of Medicine
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Dana-Farber Cancer Institute
Rapid behavior-based identification of neuroactive small molecules in the zebrafish.
Harvard Medical School
Design, synthesis and selection of DNA-encoded small-molecule libraries.
Praecis Pharmaceuticals
A new screening assay for allosteric inhibitors of cSrc.
Chemical Genomics Centre Of The Max Planck Society
Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: quinone oxidoreductase-1 (NQO1).
University Of Manchester
5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity.
Wyeth Research
Structure-based virtual screening for novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase and their experimental evaluation.
Northern Kentucky University