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 published an article on February 15 ,2020. The article was titled 《Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Electric Literature of C6H12N2O The information in the text is summarized as follows:
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 4-((4-(1H-tetrazol-1-yl)phenoxy)methyl)-2-(1-(5-ethylpyrimidin-2-yl)1,2,3,6-tetrahydropyridin-4-yl)thiazole (EC50 = 4.9 nM) and 2-(1-(5-ethylpyrimidin-2-yl)-1,2,3,6-tetrahydropyridin-4-yl)-4-((2-fluoro-4(1H-tetrazol-1-yl)phenoxy)methyl)thiazole (EC50 = 8.8 nM) with high GPR119 agonism activity and moderate clog P. Through single and long-term pharmacodynamic experiments, compound 4-((4-(1H-tetrazol-1-yl)phenoxy)methyl)-2-(1-(5-ethylpyrimidin-2-yl)1,2,3,6-tetrahydropyridin-4-yl)thiazole 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 4-((4-(1H-tetrazol-1-yl)phenoxy)methyl)-2-(1-(5-ethylpyrimidin-2-yl)1,2,3,6-tetrahydropyridin-4-yl)thiazole was a potential potent GPR119 agonist in allusion to T2DM treatment. The experimental part of the paper was very detailed, including the reaction process of Piperidine-4-carboxamide(cas: 39546-32-2Electric Literature of C6H12N2O)
Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Electric Literature of C6H12N2O
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem