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  • Title: Biscoumarin-1,2,3-triazole hybrids as novel anti-diabetic agents: Design, synthesis, in vitro α-glucosidase inhibition, kinetic, and docking studies.
    Author: Asgari MS, Mohammadi-Khanaposhtani M, Kiani M, Ranjbar PR, Zabihi E, Pourbagher R, Rahimi R, Faramarzi MA, Biglar M, Larijani B, Mahdavi M, Hamedifar H, Hajimiri MH.
    Journal: Bioorg Chem; 2019 Nov; 92():103206. PubMed ID: 31445191.
    Abstract:
    A novel series of biscoumarin-1,2,3-triazole hybrids 6a-n was prepared and evaluated for α-glucosidase inhibitory potential. All fourteen derivatives exhibited excellent α-glucosidase inhibitory activity with IC50 values ranging between 13.0 ± 1.5 and 75.5 ± 7.0 µM when compared with the acarbose as standard inhibitor (IC50 = 750.0 ± 12.0 µM). Among the synthesized compounds, compounds 6c (IC50 = 13.0 ± 1.5 µM) and 6g (IC50 = 16.4 ± 1.7 µM) exhibited the highest inhibitory activity against α-glucosidase and were non-cytotoxic towards normal fibroblast cells. Kinetic study revealed that compound 6c inhibits the α-glucosidase in a competitive mode. Furthermore, molecular docking investigation was performed to find interaction modes of the biscoumarin-1,2,3-triazole derivatives.
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