870822-95-0Relevant academic research and scientific papers
Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists
Shu, Shuangjie,Cai, Xiaoqing,Li, Jia,Feng, Yang,Dai, Antao,Wang, Jiang,Yang, Dehua,Wang, Ming-Wei,Liu, Hong
, p. 2852 - 2863 (2016)
Glucagon receptor antagonists possess a great potential for treatment of type 2 diabetes mellitus. A series of pyrazole-containing derivatives were designed, synthesized and evaluated by biological assays as glucagon receptor antagonists. Most of the compounds exhibited good in vitro efficacy. Two of them, compounds 17f and 17k, displayed relatively potent antagonist effects on glucagon receptors with IC50 values of 3.9 and 3.6 μM, respectively. The possible binding modes of 17f and 17k with the cognate receptor were explored by molecular docking simulation.
