Design of small molecule ketoamide-based inhibitors of cathepsin K

…, JA Payne, KJ Wells-Knecht, LL Wright

Index: Catalano, John G.; Deaton, David N.; Long, Stacey T.; McFadyen, Robert B.; Miller, Larry R.; Payne, J. Alan; Wells-Knecht, Kevin J.; Wright, Lois L. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 3 p. 719 - 722

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Citation Number: 27

Abstract

A novel series of ketoamide-based inhibitors of cathepsin K has been identified. Modifications to P2 and P3 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.