Author/Authors :
Alan D. Adams، نويسنده , , Winston Yuen، نويسنده , , Zao Hu، نويسنده , , Conrad Santini، نويسنده , , A. Brian Jones، نويسنده , , Karen L. MacNaul، نويسنده , , Joel P. Berger، نويسنده , , Thomas W. Doebber، نويسنده , , David E. Moller، نويسنده ,
Abstract :
A series of amphipathic 3-phenylbenzisoxazoles were found to be potent agonists of human PPARα, γ and δ. The optimization of acid proximal structure for in vitro and in vivo potency is described. Results of po dosed efficacy studies in the db/db mouse model of type 2 diabetes showed efficacy equal or superior to Rosiglitazone in correcting hyperglycemia and hypertriglyceridemia. Good functional receptor selectivity for PPARα and γ over PPARδ can be obtained.
