Altmann, Eva, Aichholz, Reiner, Betschart, Claudia, Buhl, Thomas, Green, Jonathan, Lattmann, Rene and Missbach, Martin (2006) Dipeptide nitrile inhibitors of cathepsin K. Bioorganic & Medicinal Chemistry Letters, 16 (9). pp. 2549-2554. ISSN 0960-894X

Abstract

A series of dipeptidyl nitriles as inhibitors of cathepsin K have been explored starting from lead structure 1 (Cbz-Leu-NH-CH2-CN, IC50 = 39 nM). Attachment of non-natural amino acid side chains in P1 and modification of the P3 subunit led to inhibitors with higher potency and improved pharmacokinetic properties.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.01.104
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.01.104
Date Deposited:	14 Dec 2009 14:00
Last Modified:	31 Jan 2013 01:17
URI:	https://oak.novartis.com/id/eprint/430