Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors

…, R Betageri, MJ Emmanuel, MH Hao, E Hickey…

文献索引：Bekkali, Younes; Thomson, David S.; Betageri, Raj; Emmanuel, Michel J.; Hao, Ming-Hong; Hickey, Eugene; Liu, Weimin; Patel, Usha; Ward, Yancey D.; Young, Erick R.R.; Nelson, Richard; Kukulka, Alison; Brown, Maryanne L.; Crane, Kathy; White, Della; Freeman, Dorothy M.; Labadia, Mark E.; Wildeson, Jessi; Spero, Denice M. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2465 - 2469

全文：HTML全文

被引用次数: 15

摘要

The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.