2. Academic Validation
  3. 5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents

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

  • Bioorg Med Chem Lett. 2003 Aug 18;13(16):2795-8. doi: 10.1016/s0960-894x(03)00505-5.
Ranjit C Desai 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA. [email protected]
PMID: 12873517 DOI: 10.1016/s0960-894x(03)00505-5
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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