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Bioorg Med Chem Lett. 2011 Aug 1;21(15):4409-15. doi: 10.1016/j.bmcl.2011.06.045. Epub 2011 Jun 17.

Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.

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1
GlaxoSmithKline, King of Prussia, PA 19406, United States. Jeffrey.K.Kerns@gsk.com

Abstract

A series of azepanone inhibitors of cathepsin S is described. Selectivity over both cathepsin K and cathepsin L was achieved by varying the P2 substituent. Ultimately, a balanced potency and selectivity profile was achieved in compound 39 possessing a 1-methylcyclohexyl alanine at P2 and nicotinamide as the P' substituent. The cellular potency of selected analogs is also described.

PMID:
21733692
DOI:
10.1016/j.bmcl.2011.06.045
[Indexed for MEDLINE]
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