Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
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Tully, David, Liu, Hong, Alper, Phillip, Chatterjee, Arnab, Epple, Robert, Roberts, Michael, Williams, Jennifer, Nguyen, Khanhlinh, Woodmansee, David, Tumanut, Christine, Li, Jun, Spraggon, Glen, Chang, Jonathan, Tuntland, Tove, 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.
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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 |