Title of article
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors
Author/Authors
Mimi L. Quan، نويسنده , , Christopher D. Ellis، نويسنده , , Ming Y. He، نويسنده , , Ann Y. Liauw، نويسنده , , Francis J. Woerner، نويسنده , , Richard S. Alexander، نويسنده , , Robert M. Knabb، نويسنده , , Patrick Y. S. Lam، نويسنده , , Joseph M. Luettgen، نويسنده , , Pancras C. Wong، نويسنده , , Matthew R. Wright، نويسنده , , Ruth R. Wexler، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
5
From page
369
To page
373
Abstract
Factor Xa (fXa) is an important serine protease that holds the central position linking the intrinsic and extrinsic activation mechanisms in the blood coagulation cascade. Therefore, inhibition of fXa has potential therapeutic applications in the treatments of both arterial and venous thrombosis. Herein we describe a series of tetrazole fXa inhibitors containing benzamidine mimics as the P1 substrate, of which the aminobenzisoxazole moiety was found to be the most potent benzamidine mimic. SR374 (12) inhibits fXa with a Ki value of 0.35 nM and is very selective for fXa over thrombin and trypsin.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792925
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