Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 19, Pages 2187-2191Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(00)00430-3
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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.
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