Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene

…, JA Caravella, L Chen, KL Creech, DN Deaton…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 4 p. 1206 - 1213

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被引用次数: 28

摘要

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.