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双香豆素-1,2,3-三唑杂合体作为新型抗糖尿病药物：设计、合成、体外α-葡萄糖苷酶抑制、动力学和对接研究。

Biscoumarin-1,2,3-triazole hybrids as novel anti-diabetic agents: Design, synthesis, in vitro α-glucosidase inhibition, kinetic, and docking studies.

机构信息

School of Chemistry, College of Science, University of Tehran, Tehran, Iran.

Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.

出版信息

Bioorg Chem. 2019 Nov;92:103206. doi: 10.1016/j.bioorg.2019.103206. Epub 2019 Aug 16.

DOI:10.1016/j.bioorg.2019.103206
PMID:31445191
Abstract

A novel series of biscoumarin-1,2,3-triazole hybrids 6a-n was prepared and evaluated for α-glucosidase inhibitory potential. All fourteen derivatives exhibited excellent α-glucosidase inhibitory activity with IC values ranging between 13.0 ± 1.5 and 75.5 ± 7.0 µM when compared with the acarbose as standard inhibitor (IC = 750.0 ± 12.0 µM). Among the synthesized compounds, compounds 6c (IC = 13.0 ± 1.5 µM) and 6g (IC = 16.4 ± 1.7 µM) exhibited the highest inhibitory activity against α-glucosidase and were non-cytotoxic towards normal fibroblast cells. Kinetic study revealed that compound 6c inhibits the α-glucosidase in a competitive mode. Furthermore, molecular docking investigation was performed to find interaction modes of the biscoumarin-1,2,3-triazole derivatives.

摘要

我们合成了一系列新型的二苯并吡喃-1,2,3-三唑杂合体 6a-n，并评估了它们对α-葡萄糖苷酶抑制潜力。与阿卡波糖（标准抑制剂，IC50=750.0 ± 12.0 μM）相比，这 14 种衍生物均表现出优异的α-葡萄糖苷酶抑制活性，IC50 值在 13.0 ± 1.5 和 75.5 ± 7.0 μM 之间。在所合成的化合物中，化合物 6c（IC50=13.0 ± 1.5 μM）和 6g（IC50=16.4 ± 1.7 μM）对α-葡萄糖苷酶表现出最高的抑制活性，且对正常成纤维细胞无细胞毒性。动力学研究表明，化合物 6c 以竞争性模式抑制α-葡萄糖苷酶。此外，还进行了分子对接研究，以找到二苯并吡喃-1,2,3-三唑衍生物的相互作用模式。

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