1. Syntheses and bioactivities of songorine derivatives as novel G protein-coupled receptor antagonists.
- Author
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Wang J, Bian C, Wang Y, Shen Q, Bao B, Fan J, Zuo A, Wu W, and Guo R
- Subjects
- Aconitum chemistry, Aconitum metabolism, Alkaloids metabolism, Inhibitory Concentration 50, Receptors, G-Protein-Coupled metabolism, Structure-Activity Relationship, Alkaloids chemistry, Receptors, G-Protein-Coupled antagonists & inhibitors
- 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 IC
50 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., (Copyright © 2019 Elsevier Ltd. All rights reserved.)- Published
- 2019
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