Design and synthesis of potent and subtype-selective PPARα agonists

Beginning with a moderately potent PPARγ agonist 9, a series of potent and highly subtype-selective PPARα agonists was identified through a systematic SAR study. Based on the results of the efficacy studies in the hamster and dog models of dyslipidemia and the desired pharmacokinetic data, the optimized compound 39 was selected for further profiling.

Graphical abstractA series of potent and subtype-selective PPARα agonists was synthesized. The optimized compound 39 was selected for further profiling.Figure optionsDownload full-size imageDownload as PowerPoint slide