A novel series of 1,6-bis-triazole-benzyl-α-glucoside derivatives (7a-7ee) were designed, synthesized and evaluated for inhibitory activity against α-glucosidase. Most of the synthesized compounds exhibited good activity with IC₅₀ ranging from 3.73 µM to 53.34 µM and are more potent than the standard drug acarbose (IC₅₀ = 146.25 ± 0.40 µM). SARs study showed the ester and menthol moiety play an important role in the inhibitory activity. The molecular docking model of the potent compounds 7f, 7z, 7cc and 7dd showed good binding energy and interacts well with amino acid residues around the active site of the enzyme, which confirmed the in vitro activity results.

设计、合成了一系列新的 1,6-双-三唑-苄基-α-葡萄糖苷衍生物 ( 7a-7ee )，并评估了其对α-葡萄糖苷酶的抑制活性。大多数合成化合物表现出良好的活性，IC ₅₀范围为 3.73 µM 至 53.34 µM，比标准药物阿卡波糖 (IC ₅₀  = 146.25 ± 0.40 µM)更有效。SARs研究表明酯和薄荷醇部分在抑制活性中起重要作用。强效化合物7f、7z、7cc和7dd的分子对接模型显示出良好的结合能并与酶活性位点周围的氨基酸残基相互作用良好，这证实了体外活性结果。