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.
引用
收藏
页码：1445 / 1449
页数：5
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