870823-03-3Relevant articles and documents
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities
Shu, Shuangjie,Dai, Antao,Wang, Jiang,Wang, Bin,Feng, Yang,Li, Jia,Cai, Xiaoqing,Yang, Dehua,Ma, Dakota,Wang, Ming-Wei,Liu, Hong
, p. 1896 - 1908 (2018)
A novel series of 4-methyl substituted pyrazole derivatives were designed, synthesized and biologically evaluated as potent glucagon receptor (GCGR) antagonists. In this study, compounds 9q, 9r, 19d and 19e showed high GCGR binding (IC50 = 0.09 μM, 0.06 μM, 0.07 μM and 0.08 μM, respectively) and cyclic-adenosine monophosphate (cAMP) activities (IC50 = 0.22 μM, 0.26 μM, 0.44 μM and 0.46 μM, respectively) in cell-based assays. Most importantly, the docking experiment demonstrated that compound 9r formed extensive hydrophobic interactions with the receptor binding pocket, making it justifiable to further investigate the potential of becoming a GCGR antagonist.
Pyrazole derivatives, compositions containing such compounds and methods of use
-
Page/Page column 25, (2008/06/13)
Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.