647000-54-2Relevant academic research and scientific papers
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists
Zhang, Hao,Ding, Charles Z.,Lai, Zhi,Chen, Sean S.,Devasthale, Pratik,Herpin, Tim,Morton, George,Qu, Fucheng,Ryono, Denis,Smirk, Rebecca,Wang, Wei,Wu, Shung,Ye, Xiang-Xang,Li, Yi-Xin,Apedo, Atsu,Farrelly, Dennis,Wang, Tao,Gu, Liqun,Morgan, Nathan,Flynn, Neil,Chu, Cuixia,Kunselman, Lori,Lippy, Jonathan,Locke, Kenneth,O'Malley, Kevin,Harrity, Thomas,Cap, Michael,Zhang, Lisa,Hosagrahara, Vinayak,Kadiyala, Pathanjali,Xu, Carrie,Doweyko, Arthur M.,Zahler, Robert,Hariharan, Narayanan,Cheng, Peter T.W.
, p. 1196 - 1205 (2015)
The design, synthesis and structure-activity relationships of a novel series of 3,4-disubstituted pyrrolidine acid analogs as PPAR ligands is outlined. In both the 1,3- and 1,4-oxybenzyl pyrrolidine acid series, the preferred stereochemistry was shown to be the cis-3R,4S isomer, as exemplified by the potent dual PPARα/γ agonists 3k and 4i. The N-4-trifluoromethyl-pyrimidinyl pyrrolidine acid analog 4i was efficacious in lowering fasting glucose and triglyceride levels in diabetic db/db mice.
