Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors

被引：24
|
作者：
Lubisch, W [1 ]
Hofmann, HP [1 ]
Treiber, HJ [1 ]
Möller, A [1 ]
机构：
[1] KNOLL AG, Dept Discovery Res, D-67008 Ludwigshafen, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 19期
关键词：
D O I：
10.1016/S0960-894X(00)00430-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Calpain inhibitors which are derived from piperidine carboxamides in the P-2 legion were prepared and evaluated for mu-calpain inhibition. In particular, the keto amides 11f and 11j have K-i of 30 and 9 nM and display a more than 100-fold selectivity over the closely related cysteine protease cathepsin B. Furthermore, these compounds inhibit NMDA induced convulsions in mice indicating that calpain inhibition in brain results in some anticonvulsive properties. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2187 / 2191
页数：5
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