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