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

@article{Zhang2009DesignSA,
  title={Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.},
  author={Hao Zhang and Denis Evan Ryono and Pratik Devasthale and Weiqi Wang and Kevin M. O'Malley and Dennis Farrelly and Liqun Gu and Thomas W. Harrity and Michael Cap and Cuixia Chu and Kenneth T. Locke and Litao Zhang and Jonathan S Lippy and Lori K Kunselman and Nathan N. Morgan and Neil T Flynn and Lisa Moore and Vinayak P. Hosagrahara and Lisa J Zhang and Pathanjali Kadiyala and Carrie Wenjing Xu and Arthur M. Doweyko and Aneka Bell and Chiehying J Chang and Jodi K. Muckelbauer and Robert L Zahler and Narayanan Hariharan and Peter T. W. Cheng},
  journal={Bioorganic & medicinal chemistry letters},
  year={2009},
  volume={19 5},
  pages={
          1451-6
        }
}
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. 
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