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Discovery of thiophene‐containing biaryl amide derivatives as novel glucagon receptor antagonists
Author(s) -
Li Jia,
Feng Yang,
Li Huihui,
Shu Shuangjie,
Dai Antao,
Cai Xiaoqing,
Wang Jiang,
Yang Dehua,
Ma Dakota,
Wang MingWei,
Liu Hong
Publication year - 2018
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13184
Subject(s) - glucagon receptor , thiophene , amide , chemistry , receptor , combinatorial chemistry , glucagon , binding site , stereochemistry , biochemistry , organic chemistry , hormone
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 ( IC 50 = 6.1 and 4.4 μ m , respectively) and cAMP functional activities ( IC 50 = 4.4 and 14.4 μ m , respectively). The possible binding modes of compounds 14f and 14h with GCGR were explored by molecular simulation.