Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR alpha/gamma activators.

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Ushiroda K, Maruta K, Takazawa T, Nagano T, Taiji M, Kohno T, Sato Y, Horai S, Yanagi K, Nagata R

Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR alpha/gamma activators.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):1978-82. doi: 10.1016/j.bmcl.2011.02.032. Epub 2011 Feb 13.

PubMed ID

21377875 [View in PubMed

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Abstract

In our search for new PPARalpha/gamma agonists, we designed and synthesized a series of benzoylazole-based carboxylic acids. Compound 9 showed potent PPARgamma partial agonistic activity with modest PPARalpha 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 PPARgamma full agonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pioglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	390	N/A	N/A	Details