Inhibition of α-glucosidase is an effective strategy for controlling post-prandial hyperglycemia in diabetic patients. Beside these α-glucosidase inhibitors has been also used as anti-obesity and anti-viral drugs. Keeping in view the greater importance of α-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1–20) synthesis, characterized by different spectroscopic techniques including ¹H NMR and EI-MS and their α-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC₅₀ values ranging between 1.25 ± 0.05 and 268.36 ± 4.22 µM when compared with the standard drug acarbose having IC₅₀ value 895.09 ± 2.04 µM. Our study identifies novel series of potent α-glucosidase inhibitors and further investigation on this may led to the lead compounds. A structure activity relationship has been established for all compounds. The interactions of the active compounds and enzyme active site were established with the help of molecular docking studies.

抑制α-葡萄糖苷酶是控制糖尿病患者餐后高血糖的有效策略。除了这些α-葡萄糖苷酶抑制剂外，还被用作抗肥胖和抗病毒药物。考虑到α-葡萄糖苷酶抑制剂在本研究中的重要性，我们在此介绍基于氧吲哚的恶二唑杂合类似物（1-20）的合成，其特征在于不同的光谱技术，包括¹ H NMR和EI-MS及其对α-葡萄糖苷酶的抑制活性。与具有IC的标准药物阿卡波糖相比，所有化合物均被认为是该酶的有效抑制剂，IC ₅₀值在1.25±0.05至268.36±4.22 µM之间。₅₀值895.09±2.04 µM。我们的研究确定了一系列新的有效的α-葡萄糖苷酶抑制剂，对此的进一步研究可能导致了先导化合物的产生。已经为所有化合物建立了结构活性关系。借助分子对接研究建立了活性化合物与酶活性位点之间的相互作用。