| Literature DB >> 30926314 |
Jiangming Wang1, Changhao Bian1, Yinan Wang1, Quan Shen1, Bin Bao1, Junting Fan2, Aixue Zuo3, Wenhui Wu4, Ruihua Guo5.
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 of Songorine derivatives were synthesized and their inhibitory activities on GPCRs were also evaluated by using the Double Antibody Sandwich ELISA (DAS-ELISA) in vitro. Among them, three derivatives (3a, 4, 7) exhibited significant inhibitory activity against GPCRs with IC50 values of 0.08-0.29 nM. Moreover, the structure-activity relationships (SARs) of songorine derivatives were discussed in detail. They have great potentials as novel GPCRs antagonists in the future.Entities:
Keywords: Derivatives; G protein-coupled receptors; Inhibition; Songorine; Synthesis
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Year: 2019 PMID： 30926314 DOI： 10.1016/j.bmc.2019.03.045
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641