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

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 th...

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Veröffentlicht in:Journal of biochemical and molecular toxicology 2021-04, Vol.35 (4), p.e22688-n/a
Hauptverfasser: Abedinifar, Fahimeh, Mohammadi‐Khanaposhtani, Maryam, Asemanipoor, Nafise, Mojtabavi, Somayeh, Faramarzi, Mohammad A., Mahdavi, Mohammad, Biglar, Mahmood, Larijani, Bagher, Hamedifar, Haleh, Hajimiri, Mir H.
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Sprache:eng
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Zusammenfassung: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.
ISSN:1095-6670
1099-0461
DOI:10.1002/jbt.22688