Peptidyl α-Ketoamides with Nucleobases, Methylpiperazine, and Dimethylaminoalkyl Substituents as Calpain Inhibitors

…, CY Hampton, SA Asress, FM Fernández…

Index: Ovat, Asli; Li, Zhao Zhao; Hampton, Christina Y.; Asress, Seneshaw A.; Fernandez, Facundo M.; Glass, Jonathan D.; Powers, James C. Journal of Medicinal Chemistry, 2010 , vol. 53, # 17 p. 6326 - 6336

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Citation Number: 24

Abstract

A series of peptidyl α-ketoamides with the general structure Cbz-l-Leu-d, l-AA-CONH-R were synthesized and evaluated as inhibitors for the cysteine proteases calpain I, calpain II, and cathepsin B. Nucleobases, methylpiperazine, and dimethylaminoalkyl groups were incorporated into the primed region of the inhibitors to generate compounds that potentially cross the blood− brain barrier. Two of these compounds (Cbz-Leu-d, l-Abu-CONH-(CH2) ...