Document Report Card

ID: ALA1144356

Journal: J Med Chem

Title: Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.

Authors: Shi GQ, Dropinski JF, Zhang Y, Santini C, Sahoo SP, Berger JP, Macnaul KL, Zhou G, Agrawal A, Alvaro R, Cai TQ, Hernandez M, Wright SD, Moller DE, Heck JV, Meinke PT.

Abstract: The design and synthesis of a novel class of 2,3-dihydrobenzofuran-2-carboxylic acids as highly potent and subtype-selective PPARalpha agonists are reported. Systematic study of structure-activity relationships has identified several key structural elements within this class for maintaining the potency and subtype selectivity. Select compounds were evaluated in animal models of dyslipidemia using Syrian hamsters and male Beagle dogs, and all these compounds displayed excellent cholesterol- and triglyceride-lowering activity at dose levels that were much lower than the marketed weak PPARalpha agonist fenofibrate.

CiteXplore: 16107159

DOI: 10.1021/jm050373g