- FXR agonist activity of conformationally constrained analogs of GW 4064.
FXR agonist activity of conformationally constrained analogs of GW 4064.
Bioorganic & medicinal chemistry letters (2009-07-10)
Adwoa Akwabi-Ameyaw, Jonathan Y Bass, Richard D Caldwell, Justin A Caravella, Lihong Chen, Katrina L Creech, David N Deaton, 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
PMID19586769
ABSTRACT
Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.
MATERIALS