Fang, Yuanying; Zhang, Shaokun; Li, Min; Xiong, Lijuan; Tu, Liangxing; Xie, Saisai; Jin, Yi; Liu, Yanhua; Yang, Zunhua; Liu, Ronghua published the artcile< Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists>, Application of C5H4Cl2N2O, the main research area is dihydropyrimido oxazine derivative preparation GPR 119 agonist diabetes; GPR 119 agonists; Optimisation; pyrimidodihydrooxazine; type 2 diabetes mellitus.
GPR119 is a promising target for discovery of anti-type 2 diabetes mellitus agents. We described the optimization of a novel series of pyrimido[5,4-b][1,4]oxazine derivatives as GPR119 agonists. Most designed compounds exhibited good agonistic activities. Among them, compound and demonstrated the potent EC50 values (13 and 12 nM, resp.) and strong inherent activities. Moreover, significant hypoglycemic effect of compound was observed by reducing the blood glucose AUC0-2h at the dose of 30 mg/kg, which is stronger than Vildagliptin (23.4% reduction vs. 17.9% reduction).
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antidiabetic agents. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Application of C5H4Cl2N2O.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia