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Synthesis and Biological Evaluation of a New Series of Benzofuran-1,3,4-Oxadiazole Containing 1,2,3-Triazole-Acetamides As Potential Α-Glucosidase Inhibitors Publisher Pubmed



Abedinifar F1 ; Mohammadikhanaposhtani M2 ; Asemanipoor N1 ; Mojtabavi S3 ; Faramarzi MA3 ; Mahdavi M1 ; Biglar M1 ; Larijani B1 ; Hamedifar H4 ; Hajimiri MH5
Authors

Source: Journal of Biochemical and Molecular Toxicology Published:2021


Abstract

A series of new benzofuran-1,3,4-oxadiazole containing 1,2,3-triazole-acetamides 12a-n as potential anti-α-glucosidase agents were designed and synthesized. α-Glucosidase inhibition assay demonstrated that all the synthesized compounds 12a-n (half-maximal inhibitory concentration [IC50] values in the range of 40.7 ± 0.3–173.6 ± 1.9 μM) were more potent than standard inhibitor acarbose (IC50 = 750.0 ± 12.5 µM). Among them, the most potent compound was compound 12c, with inhibitory activity around 19-fold higher than acarbose. Since the most potent compound inhibited α-glucosidase in a competitive mode, a docking study of this compound was also performed into the active site of α-glucosidase. In vitro and in silico toxicity assays of the title compounds were also performed. © 2020 Wiley Periodicals LLC
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