| Literature DB >> 18621523 |
Adwoa Akwabi-Ameyaw1, Jonathan Y Bass, Richard D Caldwell, Justin A Caravella, Lihong Chen, Katrina L Creech, David N Deaton, Stacey A Jones, Istvan Kaldor, Yaping Liu, Kevin P Madauss, Harry B Marr, Robert B McFadyen, Aaron B Miller, Frank Navas, Derek J Parks, Paul K Spearing, Dan Todd, Shawn P Williams, G Bruce Wisely.
Abstract
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the severity of cholestasis in the ANIT acute cholestatic rat model.Entities:
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Year: 2008 PMID: 18621523 DOI: 10.1016/j.bmcl.2008.06.073
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823