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Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.

Liu, Hong and Tully, David and Epple, Robert and Bursulaya, Badry and Li, Jun and Harris, Jennifer and Williams, Jennifer and Russo, Ross and Tumanut, Christine and Roberts, Michael and Alper, Phillip and He, Yun and Karanewsky, Donald (2005) Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1. Bioorganic & Medicinal Chemistry Letters, 15 (22). pp. 4979-4984. ISSN 0960-894X

Abstract

A series of Nalpha-acyl-alpha-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (Ki=3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Cathepsin S; Cathepsin; Cysteine protease inhibitor; Peptidomimetics; Noncovalent inhibitors
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Date Deposited: 14 Dec 2009 14:02
Last Modified: 31 Jan 2013 01:23
URI: https://oak.novartis.com/id/eprint/245

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