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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
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Authors Affiliations
  1. 1. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  3. 3. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. CinnaGen Medical Biotechnology Research Center, Alborz University of Medical Sciences, Karaj, Iran
  5. 5. Nano Alvand Company, Avicenna Tech Park, Tehran University of Medical Sciences, Tehran, Iran

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