Novel peptidyl α-keto amide inhibitors of calpains and other cysteine proteases

Z Li, AC Ortega-Vilain, GS Patil, DL Chu…

Index: Li, Zhaozhao; Ortega-Vilain, Anne-Cecile; Patil, Girish S.; Chu, Der-Lun; Foreman; Eveleth, David D.; Powers, James C. Journal of Medicinal Chemistry, 1996 , vol. 39, # 20 p. 4089 - 4098

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Citation Number: 155

Abstract

A series of new dipeptidyl α-keto amides of the general structure R1-l-Leu-d, l-AA-CONH-R2 were synthesized and evaluated as inhibitors for the cysteine proteases calpain I, calpain II, and cathepsin B. They combine 10 different N-protecting groups (R1), 3 amino acids residues in P1 (AA), and 44 distinct substituents on the α-keto amide nitrogen (R2). In general, calpain II was more sensitive to these inhibitors than calpain I, with a large ...

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