Abstract

Dipeptide and tripeptide aldehydes have been evaluated as inhibitors of human calpain I. Dipeptide aldehydes are generally equipotent with tripeptide aldehydes. Calpain I possesses a rather stringent requirement for Leu at P 2, but accepts a variety of capping groups and amino acids at P 1 and P 3. Several new peptide aldehydes that are more potent than previously reported calpain I inhibitors have been identified.

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