Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics

Four new peptidyl aldehydes bearing proline mimetics at the P-2-Position were synthesized and studied as inhibitors of calpain 1, cathepsin B, and selected serine proteases. The ring size of the P-2-constraining residue influenced the inhibitory potency and selectivity of the compounds for calpain I compared to the other proteases. (C) 2003 Elsevier Science Ltd. All rights reserved.