Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors

被引：52

作者：

Buckman, BO ^{[1
]}

Mohan, R ^{[1
]}

Koovakkat, S ^{[1
]}

Liang, A ^{[1
]}

Trinh, L ^{[1
]}

Morrissey, MM ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(98)00386-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

The synthesis of amidinoaryloxy 9-benzyl-8-methyl-9H-purine, 7,8-dihydropteridine-6(5H)-one and 5,7-dihydropyrimido[4,5-b][1,4]oxazine-6-one inhibitors of Factor Xa is described. These compounds show nanomolar potency against FXa and maintain high selectivity over thrombin and trypsin. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2235 / 2240

页数：6

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