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Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.

Alper, Phillip and Liu, Hong and Chatterjee, Arnab and Nguyen, Khanhlinh and Tully, David and Tumanut, Christine and Li, Jun and Harris, Jennifer and Tuntland, Tove and Chang, Jonathan and Gordon, Perry and Hollenbeck, Thomas and Karanewsky, Donald (2006) Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl. Bioorganic & Medicinal Chemistry Letters, 16 (6). pp. 1486-1490. ISSN 0960-894X

Abstract

A systematic study of anilines led to the discovery of a metabolically robust fluoroindoline replacement for the alkoxy aniline toxicophore in 1. Investigations of the P1 pocket resulted in the discovery of a wide tolerance of functionality leading to the discovery of 11 as a potent and selective inhibitor of cathepsin S.

Item Type: Article
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Additional Information: can archive final draft post-refereeing; Publisher's version/PDF cannot be used
Keywords: Cathepsin S; Noncovalent protease inhibitor; SAR
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:25
URI: https://oak.novartis.com/id/eprint/167

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