Studies towards the conception of new selective PPARβ/δ ligands

In order to define new PPARβ/δ ligands, SAR study on the selective PPARβ/δ activator L-165,041 led to the identification of one key functional group for selective PPARβ/δ activation. Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARβ/δ ligand GW501516, the conception of new ligands showing good affinity for PPARβ/δ is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPARβ/δ subtype selectivity.