Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

Abstract The design, synthesis and structure–activity relationshipsof a novel series of N -phenyl-substituted pyrrole, 1,2-pyrazole and 1,2,3-triazoleacid analogsas PPAR ligands are outlined. The triazoleacid analogs3f and 4f were identified as potent dual PPARα/γ agonists both in binding and functional assays in vitro. The 3-oxybenzyl triazoleacetic acid analog3f showed excellent glucose and triglyceride lowering in diabetic db/db mice.