新型 5,6-二芳基-1,2,4-三嗪噻唑衍生物的合成、生物评价及对接研究作为一类新型的α-葡萄糖苷酶抑制剂。
Synthesis, biological evaluation, and docking studies of novel 5,6-diaryl-1,2,4-triazine thiazole derivatives as a new class of α-glucosidase inhibitors.
机构信息
Guizhou Provincial Key Laboratory of Pharmaceutics, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550004, China; Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Guizhou Medical University, Guiyang 550004, China; School of Pharmacy, Guizhou Medical University, Guiyang 550004, China.
Guizhou Provincial Key Laboratory of Pharmaceutics, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550004, China; School of Pharmacy, Guizhou Medical University, Guiyang 550004, China.
出版信息
Bioorg Chem. 2018 Aug;78:195-200. doi: 10.1016/j.bioorg.2018.03.015. Epub 2018 Mar 21.
A novel 5,6-diaryl-1,2,4-triazine thiazole derivatives (7a-7q) were synthesized and characterized by H NMR and C NMR and evaluated for their α-glucosidase inhibitory activity. All tested compounds displayed good α-glucosidase inhibitory activity with IC values ranging between 2.85 ± 0.13 and 14.19 ± 0.23 μM when compared to the standard drug acarbose (IC = 817.38 ± 6.27 μM). Compound 7i (IC = 2.85 ± 0.13 μM) exhibited the highest activity among this series of compounds. Molecular docking studies were carried out in order to investigate the binding mode of this class of compounds to α-glucosidase. This study showed that these 5,6-diaryl-1,2,4-triazine thiazole derivatives are a new class of α-glucosidase inhibitors.
一种新型的 5,6-二芳基-1,2,4-三嗪噻唑衍生物（7a-7q）被合成并通过 1H NMR 和 13C NMR 进行了表征，并对其α-葡萄糖苷酶抑制活性进行了评价。与标准药物阿卡波糖（IC=817.38±6.27μM）相比，所有测试的化合物均表现出良好的α-葡萄糖苷酶抑制活性，IC 值在 2.85±0.13μM 至 14.19±0.23μM 之间。在这一系列化合物中，化合物 7i（IC=2.85±0.13μM）表现出最高的活性。为了研究这类化合物与α-葡萄糖苷酶的结合模式，进行了分子对接研究。这项研究表明，这些 5,6-二芳基-1,2,4-三嗪噻唑衍生物是一类新型的α-葡萄糖苷酶抑制剂。
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