Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, Beijing Road, Guiyang 550004, China.
School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China.
Molecules. 2017 Oct 30;22(11):1865. doi: 10.3390/molecules22111865.
A novel series of 2-substituted-4,6-diarylpyrimidines - has been synthesized, characterized by ¹H-NMR, C-NMR and HRMS, and screened for in vitro -glucosidase inhibitory activity. The majority of the screened compounds possessed significant α-glucosidase inhibitory activity with IC values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 μM, which is more potent than the positive control α-glucosidase inhibitor acarbose (IC = 817.38 ± 6.27 μM). Among them, was found to be the most active compound against α-glucosidase with an IC of 19.6 ± 0.21 μM. In addition, molecular docking studies were carried out to explore the binding interactions of 2-substituted-4,6-diarylpyrimidine derivatives with α-glucosidase.
我们合成了一系列新型的 2-取代-4,6-二芳基嘧啶,并通过 ¹H-NMR、C-NMR 和高分辨率质谱(HRMS)对其进行了表征,同时对其体外α-葡萄糖苷酶抑制活性进行了筛选。大多数筛选出的化合物对α-葡萄糖苷酶具有显著的抑制活性,IC 值范围为 19.6 ± 0.21 至 38.9 ± 0.35 μM,其活性强于阳性对照 α-葡萄糖苷酶抑制剂阿卡波糖(IC = 817.38 ± 6.27 μM)。其中,化合物 表现出对 α-葡萄糖苷酶最强的抑制活性,IC 值为 19.6 ± 0.21 μM。此外,还进行了分子对接研究,以探索 2-取代-4,6-二芳基嘧啶衍生物与 α-葡萄糖苷酶的结合相互作用。