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

Fahimeh Abedinifar; Maryam Mohammadi-Khanaposhtani; Nafise Asemanipoor; Somayeh Mojtabavi; Mohammad A. Faramarzi; Mohammad Mahdavi; Mahmood Biglar; Bagher Larijani; Haleh Hamedifar; Mir H. Hajimiri

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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

机译：含有1,2,3-三唑 - 乙酰胺的新一系列苯并呋喃-1,3,4-氧基唑的合成及生物学评价为潜在α-葡糖苷酶抑制剂

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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 [IC_50] values in the range of 40.7 ± 0.3-173.6 ±1.9 μM) were more potent than standard inhibitor acarbose (IC_50 = 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 a-glucosidase. In vitro and in silico toxicity assays of the title compounds were also performed.

机译：设计并合成了一系列新的含1,2,3-三唑乙酰胺的苯并呋喃-1,3,4-恶二唑类抗α-葡萄糖苷酶药物。α-葡萄糖苷酶抑制试验表明，所有合成化合物12a-n（在40.7±0.3-173.6±1.9μM范围内的半最大抑制浓度[IC_50]值）比标准抑制剂阿卡波糖（IC_50=750.0±12.5μM）更有效。其中，最有效的化合物是化合物12c，其抑制活性约为阿卡波糖的19倍。由于最有效的化合物以竞争模式抑制α-葡萄糖苷酶，因此该化合物也在α-葡萄糖苷酶的活性部位进行了对接研究。还对标题化合物进行了体外和硅毒性试验。

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来源
《Journal of biochemical and molecular toxicology》 |2021年第4期|共1页
作者
Fahimeh Abedinifar; Maryam Mohammadi-Khanaposhtani; Nafise Asemanipoor; Somayeh Mojtabavi; Mohammad A. Faramarzi; Mohammad Mahdavi; Mahmood Biglar; Bagher Larijani; Haleh Hamedifar; Mir H. Hajimiri;
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作者单位

Endocrinology and Metabolism Research Center Endocrinology and Metabolism Clinical Sciences;

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原文格式 PDF
正文语种 eng
中图分类生物化学;
关键词
1; 2; 3-triazole; 1; 3; 4-oxadiazole; acetamide; benzofuran; α-glucosidase;

机译：1;2;3-三唑;1;3;4-氧代唑;乙酰胺;苯并呋喃;α-葡糖苷酶;

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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

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