Peptidic Aldehydes Based on α- and β-Amino Acids: Synthesis, Inhibition of m-Calpain, and Anti-Cataract Properties

Autor: Payne, Richard J., Brown, Karina M., Coxon, James M., Morton, James D., Lee, Hannah Yun-Young, Abell, Andrew D.
Zdroj: Australian Journal of Chemistry; 2004, Vol. 57 Issue: 9 p877-884, 8p
Abstrakt: We present a new synthesis of SJA6017 (a potent m-calpain inhibitor) and its adaptation in order to prepare analogues in which the constituent Leu and Val residues are systematically replaced with their corresponding ?-amino acids and/or the N-terminal fluorophenylsulfonyl group is replaced by a water solubilizing N-pyridin-3-ylmethoxycarbonyl group. All compounds have been assayed against m-calpain, and the best inhibitor, SJA6017, has been shown to inhibit the development of opacity in a lens culture system design to mimic cataract.
Databáze: Supplemental Index