Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.
Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia.
Bioorg Chem. 2018 Feb;76:273-280. doi: 10.1016/j.bioorg.2017.12.001. Epub 2017 Dec 2.
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 H NMR and EI-MS and their α-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC values ranging between 1.25 ± 0.05 and 268.36 ± 4.22 µM when compared with the standard drug acarbose having IC 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，它们还被用作抗肥胖和抗病毒药物。鉴于α-葡萄糖苷酶抑制剂在本研究中的重要性，我们在这里提出了基于吲哚的恶二唑杂合类似物（1-20）的合成，通过包括 H NMR 和 EI-MS 在内的不同光谱技术进行了表征，并对其α-葡萄糖苷酶抑制活性进行了研究。所有化合物均被发现是该酶的有效抑制剂，其 IC 值范围在 1.25 ± 0.05 和 268.36 ± 4.22 µM 之间，而标准药物阿卡波糖的 IC 值为 895.09 ± 2.04 µM。我们的研究确定了一系列新型的有效α-葡萄糖苷酶抑制剂，进一步的研究可能会得到先导化合物。我们对所有化合物都建立了构效关系。通过分子对接研究，确定了活性化合物与酶活性位点的相互作用。
