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Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists |
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| Authors: | Desai Ranjit C Gratale Dominick F Han Wei Koyama Hiroo Metzger Edward Lombardo Victoria K MacNaul Karen L Doebber Thomas W Berger Joel P Leung Kwan Franklin Ronald Moller David E Heck James V Sahoo Soumya P |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. ranjit_desai@merck.com |
| Abstract: | A series of novel aryloxazolidine-2,4-diones was synthesized. A structure-activity relationship study of these compounds led to the identification of potent, orally active PPAR dual alpha/gamma agonists. Based on the results of efficacy studies in the db/db mice model of type 2 diabetes and the desired pharmacokinetic parameters, compound 12 was selected for further profiling. |
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