176751-62-5Relevant academic research and scientific papers
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors
Lubisch,Hofmann,Treiber,Moeller
, p. 2187 - 2191 (2000)
Calpain inhibitors which are derived from piperidine carboxamides in the P2 region were prepared and evaluated for μ-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.
