Amphipathic 3-Phenyl-7-propylbenzisoxazoles; human PPAR γ, δ and α agonists
AD Adams, W Yuen, Z Hu, C Santini, AB Jones…
文献索引：Adams, Alan D.; Yuen, Winston; Hu, Zao; Santini, Conrad; Jones, A. Brian; MacNaul, Karen L.; Berger, Joel P.; Doebber, Thomas W.; Moller, David E. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 5 p. 931 - 935
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 ...
