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

…, CY Hampton, SA Asress, FM Fernández…

文献索引：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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被引用次数: 24

摘要

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) ...