| Literature DB >> 16876402 |
David C Tully1, Hong Liu, Arnab K Chatterjee, Phil B Alper, Robert Epple, Jennifer A Williams, Michael J Roberts, David H Woodmansee, Brian T Masick, Christine Tumanut, Jun Li, Glen Spraggon, Michael Hornsby, Jonathan Chang, Tove Tuntland, Thomas Hollenbeck, Perry Gordon, Jennifer L Harris, Donald S Karanewsky.
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.Entities:
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Year: 2006 PMID： 16876402 DOI： 10.1016/j.bmcl.2006.07.033
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823