Aryloxazolidinediones: identification of potent orally active PPAR dual α/γ agonists
作者:Ranjit C. Desai、Dominick F. Gratale、Wei Han、Hiroo Koyama、Edward Metzger、Victoria K. Lombardo、Karen L. MacNaul、Thomas W. Doebber、Joel P. Berger、Kwan Leung、Ronald Franklin、David E. Moller、James V. Heck、Soumya P. Sahoo
DOI:10.1016/s0960-894x(03)00785-6
日期:2003.10
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. (C) 2003 Published by Elsevier Ltd.