Abstract
Calpain inhibitors which are derived from piperidine carboxamides in the P 2 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.
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