Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.
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Alper, Phillip, Liu, Hong, Chatterjee, Arnab, Nguyen, Khanhlinh, Tully, David, Tumanut, Christine, Li, Jun, Harris, Jennifer, Tuntland, Tove, Chang, Jonathan, Gordon, Perry, 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 |