Design, synthesis, and structure - Activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors

被引：32

作者：

Klingler, O

Matter, H

Schudok, M

Bajaj, SP

Czech, J

Lorenz, M

Nestler, HP

Schreuder, H

Wildgoose, P

机构：

[1] Aventis Pharma Deutschland GmbH, D-65926 Frankfurt, Germany

[2] St Louis Univ, Hlth Sci Ctr, Dept Pharmacol & Physiol Sci, St Louis, MO 63110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(03)00168-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Selective inhibition of coagulation factor VIIa has recently gained attraction as interesting approach towards antithrombotic treatment. Using parallel synthesis supported by structure-based design and X-ray crystallography, we were able to identify a novel series of amidinophenylurea derivatives with remarkable affinity for factor VIIa. The most potent compound displays a K-i value of 23 nM for factor VIIa. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1463 / 1467

页数：5

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