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- Title
Discovery of thiophene‐containing biaryl amide derivatives as novel glucagon receptor antagonists.
- Authors
Li, Jia; Feng, Yang; Li, Huihui; Shu, Shuangjie; Dai, Antao; Cai, Xiaoqing; Wang, Jiang; Yang, Dehua; Ma, Dakota; Wang, Ming‐wei; Liu, Hong
- Abstract
A novel series of thiophene‐containing biaryl amide glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, 14f and 14h, exhibited good GCGR binding (IC50 = 6.1 and 4.4 μ m, respectively) and cAMP functional activities (IC50 = 4.4 and 14.4 μ m, respectively). The possible binding modes of compounds 14f and 14h with GCGR were explored by molecular simulation.
- Subjects
THIOPHENES; AROMATIC compound derivatives; GLUCAGON receptors; RECEPTOR-ligand complexes; MOLECULAR dynamics
- Publication
Chemical Biology & Drug Design, 2018, Vol 92, Issue 1, p1241
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13184