Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators

K Ushiroda, K Maruta, T Takazawa, T Nagano…

Index: Ushiroda, Kantaro; Maruta, Katsunori; Takazawa, Takeshi; Nagano, Tomokazu; Taiji, Mutsuo; Kohno, Tetsuya; Sato, Yasuhiro; Horai, Shinji; Yanagi, Kazunori; Nagata, Ryu Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 1978 - 1982

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Citation Number: 6

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.