l-374087 and Thrombosis

l-374087 has been researched along with Thrombosis* in 2 studies

Other Studies

2 other study(ies) available for l-374087 and Thrombosis

Article	Year
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. Bioorganic & medicinal chemistry letters, 2000, May-15, Volume: 10, Issue:10 A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity of these inhibitors is reported. Topics: Acetamides; Aminopyridines; Animals; Anticoagulants; Biological Availability; Dipeptides; Dogs; Drug Design; Drug Evaluation, Preclinical; Humans; Molecular Mimicry; Pyridones; Rats; Structure-Activity Relationship; Thrombin; Thrombosis	2000
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. Bioorganic & medicinal chemistry letters, 1998, Apr-07, Volume: 8, Issue:7 Replacement of the amidinopiperidine P1 group of 3-benzylsulfonylamino-6-methyl-2-pyridinone acetamide thrombin inhibitor L-373,890 (2) with a mildly basic 5-linked 2-amino-6-methylpyridine results in an equipotent compound L-374,087 (5, Ki = 0.5 nM). Compound 5 is highly selective for thrombin over trypsin, is efficacious in the rat ferric chloride model of arterial thrombosis and is orally bioavailable in dogs and cynomolgus monkeys. The structural basis for the critical importance of both methyl groups in 5 was confirmed by X-ray crystallography. Topics: Administration, Oral; Animals; Anticoagulants; Biological Availability; Chlorides; Crystallography, X-Ray; Dogs; Ferric Compounds; Kinetics; Macaca fascicularis; Models, Molecular; Molecular Structure; Pyridones; Rats; Structure-Activity Relationship; Sulfonamides; Thrombin; Thrombosis; Trypsin	1998

Article

Year

Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.

Bioorganic & medicinal chemistry letters, 2000, May-15, Volume: 10, Issue:10

A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity of these inhibitors is reported.

Topics: Acetamides; Aminopyridines; Animals; Anticoagulants; Biological Availability; Dipeptides; Dogs; Drug Design; Drug Evaluation, Preclinical; Humans; Molecular Mimicry; Pyridones; Rats; Structure-Activity Relationship; Thrombin; Thrombosis

2000

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.

Bioorganic & medicinal chemistry letters, 1998, Apr-07, Volume: 8, Issue:7

Replacement of the amidinopiperidine P1 group of 3-benzylsulfonylamino-6-methyl-2-pyridinone acetamide thrombin inhibitor L-373,890 (2) with a mildly basic 5-linked 2-amino-6-methylpyridine results in an equipotent compound L-374,087 (5, Ki = 0.5 nM). Compound 5 is highly selective for thrombin over trypsin, is efficacious in the rat ferric chloride model of arterial thrombosis and is orally bioavailable in dogs and cynomolgus monkeys. The structural basis for the critical importance of both methyl groups in 5 was confirmed by X-ray crystallography.

Topics: Administration, Oral; Animals; Anticoagulants; Biological Availability; Chlorides; Crystallography, X-Ray; Dogs; Ferric Compounds; Kinetics; Macaca fascicularis; Models, Molecular; Molecular Structure; Pyridones; Rats; Structure-Activity Relationship; Sulfonamides; Thrombin; Thrombosis; Trypsin

1998