作者: Jiangming Wang , Changhao Bian , Yinan Wang , Quan Shen , Bin Bao
DOI: 10.1016/J.BMC.2019.03.045
关键词: Aconitum brachypodum 、 G protein-coupled receptor 、 Ic50 values 、 Receptor 、 Stereochemistry 、 In vitro 、 Chemistry 、 Double antibody sandwich
摘要: Abstract Songorine isolated from Aconitum brachypodum Diels possesses prominent activity of inhibiting G protein-coupled receptors (GPCRs) in the early screening process. In this paper, a series derivatives were synthesized and their inhibitory activities on GPCRs also evaluated by using Double Antibody Sandwich ELISA (DAS-ELISA) vitro. Among them, three (3a, 4, 7) exhibited significant against with IC50 values 0.08–0.29 nM. Moreover, structure-activity relationships (SARs) songorine discussed detail. They have great potentials as novel antagonists future.