Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Persian Medicine and Pharmacy Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
Bioorg Med Chem. 2019 Dec 1;27(23):115148. doi: 10.1016/j.bmc.2019.115148. Epub 2019 Oct 15.
In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC = 90.4-246.7 µM comparing with acarbose as the standard drug (IC = 750.0 µM). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of α-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled α-glucosidase to find the interaction modes responsible for the desired inhibitory activity.
在这项工作中，设计、合成了新型二芳基咪唑-1,2,3-三唑 7a-p 的衍生物，并评估了它们对体外α-葡萄糖苷酶抑制活性。与作为标准药物的阿卡波糖（IC = 750.0 μM）相比，所有化合物均显示出在 IC = 90.4-246.7 μM 范围内的强抑制活性。在所合成的化合物中，化合物 7b、7c 和 7e 的活性约为阿卡波糖的 8 倍。这些化合物的动力学研究表明，它们是α-葡萄糖苷酶的竞争性抑制剂。还使用模型化的α-葡萄糖苷酶对化合物 7b、7c 和 7e 进行了分子对接研究，以找到负责所需抑制活性的相互作用模式。
