Novel bicyclic lactam inhibitors of thrombin:: Highly potent and selective inhibitors

被引：18
|
作者：
St-Denis, Y
Lévesque, S
Bachand, B
Edmunds, JJ
Leblond, L
Préville, P
Tarazi, M
Winocour, PD
Siddiqui, MA
机构：
[1] Shire BioChem, Laval, PQ H7V 4A7, Canada
[2] Pfizer Global Res & Dev, Ann Arbor, MI 48105 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 08期
关键词：
D O I：
10.1016/S0960-894X(02)00131-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The potency and selectivity of a previous series of low molecular weight thrombin inhibitors were improved through modifications of the P1 and P3 residues. Introduction of diphenyl substituted sulfonamides in the P3 moiety led to highly efficacious compounds. By correctly selecting the combination of P1 and P3 residues, high levels of potency, selectivity and in vivo efficacy were obtained. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1181 / 1184
页数：4
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