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

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1451-6. doi: 10.1016/j.bmcl.2009.01.030. Epub 2009 Jan 15.


The design, synthesis and structure-activity relationships of a novel series of N-phenyl-substituted pyrrole, 1,2-pyrazole and 1,2,3-triazole acid analogs as PPAR ligands are outlined. The triazole acid analogs 3f and 4f were identified as potent dual PPARalpha/gamma agonists both in binding and functional assays in vitro. The 3-oxybenzyl triazole acetic acid analog 3f showed excellent glucose and triglyceride lowering in diabetic db/db mice.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Azoles / chemical synthesis*
  • Azoles / pharmacology
  • Cell Line / enzymology
  • Crystallography, X-Ray
  • Drug Design*
  • Female
  • Humans
  • Hydrogen-Ion Concentration
  • Mice
  • Mice, Transgenic
  • PPAR alpha / agonists*
  • PPAR alpha / metabolism
  • PPAR gamma / agonists*
  • PPAR gamma / metabolism
  • Structure-Activity Relationship


  • Azoles
  • PPAR alpha
  • PPAR gamma