Title of article
Amphipathic 3-Phenyl-7-propylbenzisoxazoles; human pPaR γ, δ and α agonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
5
From page
931
To page
935
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793048
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