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

Jonathan Y. Bass,Justin A. Caravella,Lihong Chen,Katrina L. Creech,David N. Deaton,Kevin P. Madauss,Harry B. Marr,Robert B. McFadyen,Aaron B. Miller,Wendy Y. Mills,Frank Navas,Derek J. Parks,Terrence L. Smalley,Paul K. Spearing,Dan Todd,Shawn P. Williams,G. Bruce Wisely

Bioorganic & Medicinal Chemistry Letters（2011）

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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, GSK2324 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.

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关键词

Farnesoid X receptor,FXR,Nuclear receptor modulator,FXR X-ray co-crystal structure,GW 4064,GSK8062,Bile acid receptor,NR1H4 GSK2324

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