Benzoxazinones as PPARγ agonists. part 1: SAR of three aromatic regions
PJ Rybczynski, RE Zeck, DW Combs, I Turchi…
文献索引：Rybczynski, Philip J.; Zeck, Roxanne E.; Combs, Donald W.; Turchi, Ignatius; Burris, Thomas P.; Xu, Jun Z.; Yang, Maria; Demarest, Keith T. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2359 - 2362
A series of benzoxazinones was synthesized as PPARγ agonists. The compounds were obtained in seven steps, and SAR was developed by variations to the core shown below. The compounds were tested as functional agonists in the induction of the aP2 gene in preadipocytes, and the most potent compound in the series has an EC50= 0.51 μM. The potency was further confirmed through a PPAR-Gal4 construct. Efficacy has been ...
