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Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.

Tully, David and Liu, Hong and Alper, Phillip and Chatterjee, Arnab and Epple, Robert and Roberts, Michael and Williams, Jennifer and Nguyen, Khanhlinh and Woodmansee, David and Tumanut, Christine and Li, Jun and Spraggon, Glen and Chang, Jonathan and Tuntland, Tove and Harris, Jennifer and Karanewsky, Donald (2006) Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3. Bioorganic & medicinal chemistry letters, 16 (7). pp. 1975-1980. ISSN 0960-894X

Abstract

A series of N(alpha)-2-benzoxazolyl-alpha-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure-activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing)
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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/165

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