1,3,5-Trisubstituted aryls as highly selective PPARδ agonists

A series of highly potent and selective PPARδ agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 μM, making it a useful tool in studying the biological effects of selective PPARδ activation.

A series of highly potent and selective PPAR agonists is reported.Figure optionsDownload as PowerPoint slide