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Bioorg Med Chem Lett. 2016 Dec 1;26(23):5719-5723. doi: 10.1016/j.bmcl.2016.10.057. Epub 2016 Oct 21.

Synthesis and biological evaluation of novel 2,4,5-triarylimidazole-1,2,3-triazole derivatives via click chemistry as α-glucosidase inhibitors.

Author information

1
College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China. Electronic address: wanggch123@163.com.
2
College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China.

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.

KEYWORDS:

1,2,3-Triazole; 2,4,5-Triarylimidazole; Click chemistry; Enzyme kinetic study; Molecular docking; α-Glucosidase inhibitor

PMID:
27810241
DOI:
10.1016/j.bmcl.2016.10.057
[Indexed for MEDLINE]

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