Bioorganic and Medicinal Chemistry Letters (2020)
Update date:2022-08-16
Topics:
Zuo, Zeping
Chen, Miaomiao
Shao, Xiaoni
Qian, Xinying
Liu, Xiaocong
Zhou, Xia
Xiang, Jiawei
Deng, Pengchi
Li, Yan
Jie, Hui
Liu, Chunqi
Cen, Xiaobo
Xie, Yongmei
Zhao, Yinglan
A series of novel tetrahydropyridine derivatives were prepared and evaluated using cell-based measurements. Systematic optimization of general structure G-1 led to the identification of compound 35 (EC50 = 4.9 nM) and 37 (EC50 = 8.8 nM) with high GPR119 agonism activity and moderate clog P. Through single and long-term pharmacodynamic experiments, we found that compound 35 showed a hypoglycemic effect and may have an effect on improving basal metabolic rate in DIO mice. Both in vitro and in vivo tests indicated that compound 35 was a potential potent GPR119 agonist in allusion to T2DM treatment.
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