Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors

被引：114

作者：

Zhao, ZS ^{[1
]}

Arnaiz, DO ^{[1
]}

Griedel, B ^{[1
]}

Sakata, S ^{[1
]}

Dallas, JL ^{[1
]}

Whitlow, M ^{[1
]}

Trinh, L ^{[1
]}

Post, J ^{[1
]}

Liang, A ^{[1
]}

Morrissey, MM ^{[1
]}

Shaw, KJ ^{[1
]}

机构：

[1] Berlex Biosci, Discovery Res, Richmond, CA 94804 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)00139-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500-1000-fold selectivity against thrombin and 50-100-fold selectivity against trypsin. The 2-substituent on the benzimidazole ring had a strong impact on the FXa inhibitory activity. Crystallography studies suggest that the 2-substituent may have a conformational effect favoring the extended binding conformation. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：963 / 966

页数：4

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