Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists

[Display omitted] 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 moderat...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2020-02, Vol.30 (4), p.126855-126855, Article 126855
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2,3,6-Tetrahydropyridine derivatives Animals Blood Glucose - analysis Drug Design Glucose Tolerance Test GPR119 agonist Humans Hypoglycemic Agents - chemistry Hypoglycemic Agents - metabolism Hypoglycemic Agents - therapeutic use Male Mice Mice, Inbred C57BL Obesity - drug therapy Obesity - pathology OGTT Pyrrolidines - chemistry Pyrrolidines - metabolism Pyrrolidines - therapeutic use Rats Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism Solubility Structure-Activity Relationship Type 2 diabetes
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