Title of article
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors
Author/Authors
Mimi L. Quan، نويسنده , , Christopher D. Ellis، نويسنده , , Ming Y. He، نويسنده , , Ann Y. Liauw، نويسنده , , Patrick Y. S. Lam، نويسنده , , Karen A. Rossi، نويسنده , , Robert M. Knabb، نويسنده , , Joseph M. Luettgen، نويسنده , , Matthew R. Wright، نويسنده , , Pancras C. Wong، نويسنده , , Ruth R. Wexler، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
6
From page
1023
To page
1028
Abstract
Factor Xa (fXa) is an important serine protease in the blood coagulation cascade. Inhibition of fXa has emerged as an attractive target for potential therapeutic applications in the treatments of both arterial and venous thrombosis. Herein, we describe a series of non-benzamidine isoxazoline derivatives as fXa inhibitors. The chloroaniline group was found to be the most potent benzamidine mimic in this series. Chloroaniline 1 (ST368) has a Ki value of 1.5 nM against fXa and is highly selective for fXa relative to thrombin and trypsin.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793066
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