Peer-reviewed veterinary case report
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2008
- Authors:
- Akwabi-Ameyaw, Adwoa et al.
- Affiliation:
- Department of Medicinal Chemistry · United States
- Species:
- rodent
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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/18621523/