Isoxazolines and isoxazoles as Factor Xa inhibitors

被引：70

作者：

Pruitt, JR ^{[1
]}

Pinto, DJ ^{[1
]}

Estrella, MJ ^{[1
]}

Bostrom, LL ^{[1
]}

Knabb, RM ^{[1
]}

Wong, PC ^{[1
]}

Wright, MR ^{[1
]}

Wexler, RR ^{[1
]}

机构：

[1] Dupont Merck Pharmaceut Co, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)00097-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

3,4,5-Trisubstituted isoxazolines (2) and isoxazoles (3) were prepared and evaluated for their in vitro and in vivo antithrombotic efficacy. They were compared to 3,5,5-trisubstituted isoxazolines (1) for Factor Xa selectivity and potency. They were also compared in an arterio-venous (A-V) shunt model of thrombosis. (C) 2000 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

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页码：685 / 689

页数：5

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