Tully, David, Liu, Hong, Chatterjee, Arnab, Alper, Phillip, Williams, Jennifer, Roberts, Michael, Mutnick, Daniel, Woodmansee, David, Hollenbeck, Thomas, Gordon, P., Chang, Jonathan, Tuntland, Tove, Tumanut, Christine, Li, Jun, 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