Amido-(propyl and allyl)-hydroxybenzamidines: Development of achiral inhibitors of factor Xa

被引：12

作者：

Gong, Y

Pauls, HW

Spada, AP

Czekaj, M

Liang, GY

Chu, V

Colussi, DJ

Brown, KD

Gao, JB

机构：

[1] Rhone Poulenc Rorer, Dept Med Chem, Collegeville, PA 19426 USA

[2] Rhone Poulenc Rorer, Comp Assisted Drug Design, Collegeville, PA 19426 USA

[3] Rhone Poulenc Rorer, Cardiovasc Biol, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(99)00673-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design, synthesis and SAR of amido-(propyl and allyl)-hydroxybenzamidine coagulation factor Xa inhibitors is described. These achiral inhibitors are selective for fXa vis a vis structurally related serine proteases and are readily prepared in 6-7 linear steps. The most potent member 9j (fXa K-i = 0.75 nM) is selective (>1000-fold) and an effective anticoagulant in mammalian plasma. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：217 / 221

页数：5

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