Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Design, synthesis and evaluation of 3-phenoxypyrazine-2-carboxamide derivatives as potent TGR5 agonists
RSC Advances ( IF 3.9 ) Pub Date : 2022-01-27 , DOI: 10.1039/d1ra08867j Shizhen Zhao 1 , Le Wang 1 , Jie Wang 1 , Chenwei Wang 1 , Shaowei Zheng 1 , Yajie Fu 1 , Yunfu Li 1 , Wei-Dong Chen 1, 2 , Ruifang Hou 1 , Dongbin Yang 1 , Yan-Dong Wang 3
RSC Advances ( IF 3.9 ) Pub Date : 2022-01-27 , DOI: 10.1039/d1ra08867j Shizhen Zhao 1 , Le Wang 1 , Jie Wang 1 , Chenwei Wang 1 , Shaowei Zheng 1 , Yajie Fu 1 , Yunfu Li 1 , Wei-Dong Chen 1, 2 , Ruifang Hou 1 , Dongbin Yang 1 , Yan-Dong Wang 3
Affiliation
|
TGR5 is emerging as an important and promising target for the treatment of non-alcoholic steatohepatitis, type 2 diabetes mellitus (T2DM), and obesity. A series of novel 3-phenoxypyrazine-2-carboxamide derivatives were designed, synthesized and evaluated in vitro and in vivo. The most potent compounds 18g and 18k exhibited excellent hTGR5 agonist activity, which was superior to those of the reference drug INT-777. In addition, compound 18k could significantly reduce blood glucose levels in C57 BL/6 mice and stimulate GLP-1 secretion in NCI-H716 cells and C57 BL/6 mice.
中文翻译：
3-苯氧基吡嗪-2-甲酰胺衍生物作为有效 TGR5 激动剂的设计、合成和评价
TGR5 正在成为治疗非酒精性脂肪性肝炎、2 型糖尿病 (T2DM) 和肥胖症的重要且有希望的靶点。设计、合成并在体外和体内评估了一系列新型 3-苯氧基吡嗪-2-甲酰胺衍生物。最有效的化合物18g和18k表现出优异的 hTGR5 激动剂活性，优于参考药物 INT-777。此外，化合物18k可显着降低 C57 BL/6 小鼠的血糖水平，并刺激 NCI-H716 细胞和 C57 BL/6 小鼠的 GLP-1 分泌。
更新日期：2022-01-27
中文翻译：
3-苯氧基吡嗪-2-甲酰胺衍生物作为有效 TGR5 激动剂的设计、合成和评价
TGR5 正在成为治疗非酒精性脂肪性肝炎、2 型糖尿病 (T2DM) 和肥胖症的重要且有希望的靶点。设计、合成并在体外和体内评估了一系列新型 3-苯氧基吡嗪-2-甲酰胺衍生物。最有效的化合物18g和18k表现出优异的 hTGR5 激动剂活性，优于参考药物 INT-777。此外，化合物18k可显着降低 C57 BL/6 小鼠的血糖水平，并刺激 NCI-H716 细胞和 C57 BL/6 小鼠的 GLP-1 分泌。
京公网安备 11010802027423号