947330-91-8Relevant articles and documents
Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene
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)
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.
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists
Kher, Sunil,Lake, Kirk,Sircar, Ila,Pannala, Madhavi,Bakir, Farid,Zapf, James,Xu, Kui,Zhang, Shao-Hui,Liu, Juping,Morera, Lisa,Sakurai, Naoki,Jack, Rick,Cheng, Jie-Fei
, p. 4442 - 4446 (2008/02/11)
Structure-activity relationship studies on a series of Boc-indole derivatives as LXR agonists are described. Compound 1 was identified as an LXR agonist through structure-based virtual screening followed by high-throughput gene profiling. Replacement of t
