Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373568 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
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
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Younes Bekkali, David S. Thomson, Raj Betageri, Michel J. Emmanuel, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Usha Patel, Yancey D. Ward, Erick R.R. Young, Richard Nelson, Alison Kukulka, Maryanne L. Brown, Kathy Crane, Della White, Dorothy M. Freeman,