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  • Title: Synthesis and biological evaluation of novel 2,4,5-triarylimidazole-1,2,3-triazole derivatives via click chemistry as α-glucosidase inhibitors.
    Author: Wang G, Peng Z, Wang J, Li J, Li X.
    Journal: Bioorg Med Chem Lett; 2016 Dec 01; 26(23):5719-5723. PubMed ID: 27810241.
    Abstract:
    A novel series of 2,4,5-triarylimidazole-1,2,3-triazole derivatives were synthesized via copper(I)-catalyzed azide-alkyne click chemistry, and evaluated for their α-glucosidase inhibitory activity. All tested compounds showed potent α-glucosidase inhibitory activity with IC50 ranging from 15.16±0.18 to 48.15±0.37μM, in comparison to the standard drug, acarbose (IC50=817.38±6.27μM). Among all the tested compounds, 5j was found to be the most active compound with IC50 value of 15.16±0.18μM and behaved as a noncompetitive inhibitor with a Ki of 14.78μM. In addition, molecular docking study was carried out to explore the binding interactions of these compounds with α-glucosidase enzyme.
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