Design of small molecule ketoamide-based inhibitors of cathepsin K

  • Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22. doi: 10.1016/j.bmcl.2003.11.029.
John G Catalano  1 ,  David N Deaton ,  Stacey T Long ,  Robert B McFadyen ,  Larry R Miller ,  J Alan Payne ,  Kevin J Wells-Knecht ,  Lois L Wright
Affiliations
  • 1. Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
PMID: 14741275 DOI: 10.1016/j.bmcl.2003.11.029
Abstract

A novel series of ketoamide-based inhibitors of Cathepsin K has been identified. Modifications to P(2) and P(3) elements were crucial to enhancing inhibitory activity. Although not optimized, a selected inhibitor was effective in attenuating type I Collagen hydrolysis in a surrogate assay of bone resorption.

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