Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376393 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
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.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Adwoa Akwabi-Ameyaw, 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,