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  • Title: Design, synthesis, in vitro, and in silico studies of novel diarylimidazole-1,2,3-triazole hybrids as potent α-glucosidase inhibitors.
    Author: Saeedi M, Mohammadi-Khanaposhtani M, Asgari MS, Eghbalnejad N, Imanparast S, Faramarzi MA, Larijani B, Mahdavi M, Akbarzadeh T.
    Journal: Bioorg Med Chem; 2019 Dec 01; 27(23):115148. PubMed ID: 31679980.
    Abstract:
    In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC50 = 90.4-246.7 µM comparing with acarbose as the standard drug (IC50 = 750.0 µM). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of α-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled α-glucosidase to find the interaction modes responsible for the desired inhibitory activity.
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