Bioorganic and Medicinal Chemistry Letters p. 5719 - 5723 (2016)
Update date:2022-08-30
Topics:
Wang, Guangcheng
Peng, Zhiyun
Wang, Jing
Li, Juan
Li, Xin
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 IC50ranging from 15.16 ± 0.18 to 48.15 ± 0.37 μM, in comparison to the standard drug, acarbose (IC50= 817.38 ± 6.27 μM). Among all the tested compounds, 5j was found to be the most active compound with IC50value of 15.16 ± 0.18 μM and behaved as a noncompetitive inhibitor with a Kiof 14.78 μM. In addition, molecular docking study was carried out to explore the binding interactions of these compounds with α-glucosidase enzyme.
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