Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.
作者： Jonathan Y. Bass , Justin A. Caravella , Lihong Chen , Katrina L. Creech , David N. Deaton
DOI: 10.1016/J.BMCL.2010.12.089
关键词: Farnesoid X receptor 、 Quinoline 、 Chemistry 、 Agonist 、 G protein-coupled bile acid receptor 、 Nuclear receptor 、 Chemical synthesis 、 Receptor 、 Stereochemistry 、 Bicyclic molecule
摘要: To improve on the drug properties of GSK8062 1b, a series heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved developability parameters relative to 1b. In addition, analog lowered body weight gain and serum glucose in DIO mouse model diabetes.
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