A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a–k as α-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a–k against yeast α-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound 8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed that α-glucosidase inhibition of compound 8d was the competitive type. Furthermore, docking study suggested that compound 8d is more stable than acarbose in the active site of α-glucosidase.

中文翻译：

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新的邻苯二甲酰亚胺-苯甲酰胺-1,2,3-三唑杂化物; 设计，合成，α-葡萄糖苷酶抑制测定和对接研究

设计并合成了一系列新的邻苯二甲酰亚胺-苯甲酰胺-1,2,3-三唑杂合体8a-k作为α-葡萄糖苷酶抑制剂。化合物8a-k对酵母α-葡萄糖苷酶的生物学评估表明，与标准抑制剂阿卡波糖相比，它们都具有出色的抑制活性。其中，最有效的化合物是抑制活性比阿卡波糖高18.5倍的化合物8d。动力学研究表明，化合物8d的α-葡萄糖苷酶抑制是竞争型。此外，对接研究表明，化合物8d在α的活性位点比阿卡波糖更稳定。-葡糖苷酶。