Neutral inhibitors of the serine protease factor Xa

被引：25

作者：

Shrader, WD

Young, WB

Sprengeler, PA

Sangalang, JC

Elrod, K

Carr, G

机构：

[1] Axys Pharmaceut Inc, Dept Med Chem, S San Francisco, CA 94080 USA

[2] Axys Pharmaceut Inc, Dept Struct Chem & Enzymol, S San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(01)00312-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A neutral inhibitor of the serine protease factor Xa was identified via a high throughput screen of a commercial library. The initial lead 1 demonstrated reversible and competitive inhibition kinetics for factor Xa and possessed a high degree of selectivity versus other related serine proteases. Initial modeling efforts and the generation of a series of analogues of 1 are described. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1801 / 1804

页数：4

共 18 条

[1] CONFORMATIONAL-ANALYSIS .130. MM2 - HYDROCARBON FORCE-FIELD UTILIZING V1 AND V2 TORSIONAL TERMS [J].