Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
Article Details
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Adams AD, Yuen W, Hu Z, Santini C, Jones AB, MacNaul KL, Berger JP, Doebber TW, Moller DE
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
Bioorg Med Chem Lett. 2003 Mar 10;13(5):931-5.
- PubMed ID
- 12617924 [ View in PubMed]
- Abstract
A series of amphipathic 3-phenylbenzisoxazoles were found to be potent agonists of human PPARalpha, gamma and delta. 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 PPARalpha and gamma over PPARdelta can be obtained.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha Ki (nM) >33300 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor delta Ki (nM) >33300 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma Ki (nM) 136 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 21 N/A N/A Details