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Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.

Tully, David and Liu, Hong and Chatterjee, Arnab and Alper, Phillip and Epple, Robert and Williams, Jennifer and Roberts, Michael and Woodmansee, David and Masick, Brian and Tumanut, Christine and Li, Jun and Spraggon, Glen and Hornsby, Michael and Chang, Jonathan and Tuntland, Tove and Hollenbeck, Thomas and Gordon, P. and Harris, Jennifer and Karanewsky, Donald (2006) Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers. Bioorganic & Medicinal Chemistry Letters, 16 (19). pp. 5112-5117. ISSN 0960-894X

Abstract

The synthesis and structure-activity relationship of a series of arylaminoethyl amide cathepsin S inhibitors are reported. Optimization of P3 and P2 groups to improve overall physicochemical properties resulted in significant improvements in oral bioavailability over early lead compounds. An X-ray structure of compound 37 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); Publisher's version/PDF cannot be used
Keywords: Cathepsin S; Cysteine protease inhibitor; Noncovalent inhibitor; Peptidomimetic; X-ray structure
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:26
URI: https://oak.novartis.com/id/eprint/143

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