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. 2003 Mar 24;13(6):1023-8.
doi: 10.1016/s0960-894x(03)00080-5.

Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors

Mimi L Quan  1 , Christopher D Ellis, Ming Y He, Ann Y Liauw, Patrick Y S Lam, Karen A Rossi, Robert M Knabb, Joseph M Luettgen, Matthew R Wright, Pancras C Wong, Ruth R Wexler
Affiliations

Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors

Mimi L Quan et al. Bioorg Med Chem Lett. .

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 K(i) value of 1.5 nM against fXa and is highly selective for fXa relative to thrombin and trypsin.

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