Tully, David and Liu, Hong and Chatterjee, Arnab and Alper, Phillip and Williams, Jennifer and Roberts, Michael and Mutnick, Daniel and Woodmansee, David and Hollenbeck, Thomas and Gordon, P. and Chang, Jonathan and Tuntland, Tove and Tumanut, Christine and Li, Jun and Harris, Jennifer and Karanewsky, Donald (2006) Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors. Bioorganic & Medicinal Chemistry Letters, 16 (19). pp. 5107-5111. ISSN 0960-894X

Abstract

We report a novel series of noncovalent inhibitors of cathepsin S. The synthesis of the peptidomimetic scaffold is described and structure-activity relationships of P3, P1, and P1' subunits are discussed. Lead optimization to a non-peptidic scaffold has resulted in a new class of potent, highly selective, and orally bioavailable cathepsin S inhibitors.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.07.032
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	Cathepsin; Cysteine protease inhibitor; Non-covalent inhibitor; Peptidomimetic
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.07.032
Date Deposited:	14 Dec 2009 14:04
Last Modified:	31 Jan 2013 01:26
URI:	https://oak.novartis.com/id/eprint/142