Abstract α-Glucosidase enzyme is a therapeutic target for diabetes mellitus and its inhibitors play a vital role in the treatment of this disease. A new series of aryl-oxadiazole Schiff bases (1–18) were synthesized and evaluated for α-glucosidase inhibitory potential. Fifteen compounds 1–8, 11–13, and 15–18 showed excellent inhibition with IC50 values ranging from 0.30 ± 0.2 to 35.1 ± 0.80 µM as compared to the standard inhibitor acarbose (IC50 = 38.45 ± 0.80 µM), nonetheless, the remaining compounds were found to have moderate activity. Among the series, compounds 7 (IC50 = 0.30 ± 0.2 μM) with hydroxy groups at phenyl rings on either side of the oxadiazole ring was identified as the most potent inhibitor of α-glucosidase. The molecular docking studies were conducted to understand the binding mode of active inhibitors with the active site of enzyme and results supported the experimental data.

中文翻译：

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芳基恶二唑席夫碱：合成、α-葡萄糖苷酶体外抑制活性及其计算机研究

摘要 α-葡萄糖苷酶是糖尿病的治疗靶点，其抑制剂在该病的治疗中起着至关重要的作用。合成了一系列新的芳基恶二唑席夫碱 (1-18) 并评估了 α-葡萄糖苷酶抑制潜力。与标准抑制剂阿卡波糖 (IC50 = 38.45 ± 0.80 µM) 相比，15 种化合物 1–8、11–13 和 15–18 显示出极好的抑制作用，IC50 值范围为 0.30 ± 0.2 至 35.1 ± 0.80 µM，但其余的发现化合物具有中等活性。在该系列中，在恶二唑环两侧的苯环上具有羟基的化合物 7 (IC50 = 0.30 ± 0.2 μM) 被鉴定为最有效的 α-葡萄糖苷酶抑制剂。