New β-carboline derivatives as potential α-glucosidase inhibitor: Synthesis and biological activity evaluation

α-Glucosidase is an important therapeutic target of diabetes mellitus. To find potent α-glucosidase inhibitors, thirty-one β-carboline derivatives containing piperazine moieties (6a∼6u, 7a∼7j) were synthesized and evaluated their α-glucosidase inhibitory activity. Most β-carboline derivatives showed...

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Published in:Journal of molecular structure 2023-07, Vol.1283, p.135279, Article 135279
Main Authors: Lin, Jin, Xiao, Di, Lu, Li, Liang, Bingwen, Xiong, Zhuang, Xu, Xuetao
Format: Article
Language:English
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Inhibitor
Molecular docking
Spectral analysis
α-Glucosidase
β-Carboline derivatives
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description α-Glucosidase is an important therapeutic target of diabetes mellitus. To find potent α-glucosidase inhibitors, thirty-one β-carboline derivatives containing piperazine moieties (6a∼6u, 7a∼7j) were synthesized and evaluated their α-glucosidase inhibitory activity. Most β-carboline derivatives showed potential α-glucosidase inhibitory activity, especially, compound 7c presented obvious α-glucosidase inhibitory activity (IC50: 8.9 ± 0.2 μM), ∼ 69 folds stronger than acarbose (IC50: 610.7 ± 0.1 μM). Inhibition mechanism and kinetics explained compound 7c to be a reversible and mixed-type inhibitor. CD spectra, 3D fluorescence, and molecular docking were employed to reveal the mechanisms of 7c against α-glucosidase. Cell cytotoxicity assay ascertained low cytotoxicity of 7c. [Display omitted]
doi_str_mv 10.1016/j.molstruc.2023.135279
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subjects Inhibitor
Molecular docking
Spectral analysis
α-Glucosidase
β-Carboline derivatives
title New β-carboline derivatives as potential α-glucosidase inhibitor: Synthesis and biological activity evaluation
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