Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors |
| |
Authors: | Lubisch W Hofmann H P Treiber H J Möller A |
| |
Affiliation: | Department of Discovery Research, KNOLL AG, Ludwigshafen, Germany. wilfried.lubisch@knoll-ag.de |
| |
Abstract: | Calpain inhibitors which are derived from piperidine carboxamides in the P2 region were prepared and evaluated for mu-calpain inhibition. In particular, the keto amides 11f and 11j have Ki 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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |