Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene
To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.
Bass, Jonathan Y.,Caravella, Justin A.,Chen, Lihong,Creech, Katrina L.,Deaton, David N.,Madauss, Kevin P.,Marr, Harry B.,McFadyen, Robert B.,Miller, Aaron B.,Mills, Wendy Y.,Navas III, Frank,Parks, Derek J.,Smalley Jr., Terrence L.,Spearing, Paul K.,Todd, Dan,Williams, Shawn P.,Wisely, G. Bruce
supporting information; experimental part
p. 1206 - 1213
(2011/04/16)
FARNESOID X RECEPTOR AGONISTS
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Page/Page column 81
(2008/06/13)
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