High-throughput synthesis and optimization of thrombin inhibitors via urazole α-addition and Michael addition

被引：39

作者：

Boatman, PD

Urban, J

Nguyen, M

Qabar, M

Kahn, M

机构：

[1] Molecumetics, Bellevue, WA 98005 USA

[2] Pacific NW Res Inst, Seattle, WA 98122 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(03)00155-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel alpha-addition of propiolates to urazoles followed by Michael addition of a variety of nucleophiles has been developed for rapid production and optimization of peptidomimetic drug leads. This technology has produced a number of highly potent and selective inhibitors of the serine protease, thrombin. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：1445 / 1449

页数：5

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