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Probing the P3' pocket of stromelysin with piperazic acid analogs

被引：10
作者：
Nugiel, DA
Jacobs, K
Decicco, CP
Nelson, DJ
Copeland, RA
Hardman, KD
机构：
[1] The DuPont Merck Pharmaceutical Co., Wilmington, DE 19880-0353
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 24期
关键词：
D O I：
10.1016/0960-894X(95)00536-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The preparation and SAR of several piperazic acid-based stromelysin (MMP-3) inhibitors is presented. The standard P3' methyl amide substituent can be replaced by other carboxy based substituents and maintain good binding affinity. Removal of a hydrogen-bond acceptor results in a 30-fold decrease in activity.
引用
收藏
页码：3053 / 3056
页数：4
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