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5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.

Ranjit C Desai,Wei Han,Edward J Metzger,Jeffrey P Bergman,Dominick F Gratale,Karen L MacNaul,Joel P Berger,Thomas W Doebber,Kwan Leung,David E Moller,James V Heck,Soumya P Sahoo

Bioorganic & medicinal chemistry letters（2003）

Cited 73|Views11
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Abstract
A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARalpha/gamma agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.
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