Liu, Hong, Tully, David, Epple, Robert, Bursulaya, Badry, Li, Jun, Harris, Jennifer, Williams, Jennifer, Russo, Ross, Tumanut, Christine, Roberts, Michael, Alper, Phillip, 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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2005.08.017
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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2005.08.017
Date Deposited:	14 Dec 2009 14:02
Last Modified:	31 Jan 2013 01:23
URI:	https://oak.novartis.com/id/eprint/245