Article ID Journal Published Year Pages File Type
1373568 Bioorganic & Medicinal Chemistry Letters 2007 5 Pages PDF
Abstract

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.

Graphical abstractThe synthesis and SAR of the first succinyl-nitrile-based compounds as Cathepsin S inhibitors are described.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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