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  • Title: Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators.
    Author: Ushiroda K, Maruta K, Takazawa T, Nagano T, Taiji M, Kohno T, Sato Y, Horai S, Yanagi K, Nagata R.
    Journal: Bioorg Med Chem Lett; 2011 Apr 01; 21(7):1978-82. PubMed ID: 21377875.
    Abstract:
    In our search for new PPARα/γ agonists, we designed and synthesized a series of benzoylazole-based carboxylic acids. Compound 9 showed potent PPARγ partial agonistic activity with modest PPARα agonistic activity. The sodium salt of 9 (9Na) demonstrated potent efficacy in lowering both blood glucose and lipids in an animal model without causing significant body weight gain, a well-known side effect associated with PPARγ full agonists.
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