Department of Chemistry, Hazara University, Mansehra 21120, Khyber Pukhtunkhwa, Pakistan.
Department of Chemistry, Hazara University, Mansehra 21120, Khyber Pukhtunkhwa, Pakistan.
Bioorg Chem. 2015 Feb;58:81-7. doi: 10.1016/j.bioorg.2014.12.001. Epub 2014 Dec 10.
A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and (1)H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46±0.008 and 312.79±0.06 μM when compared with the standard acarbose (IC50, 38.25±0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46±0.008, 37.78±0.05, 28.91±0.0, 38.12±0.04, 37.43±0.03, 36.89±0.06 and 37.11±0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking.
合成了一系列新的三嗪并吲哚类似物 1-11，通过 EI-MS 和 (1)H NMR 进行了表征，并评估了它们对 α-葡萄糖苷酶抑制潜力。与标准阿卡波糖 (IC50，38.25±0.12 μM) 相比，这 11 种类似物均表现出不同程度的 α-葡萄糖苷酶抑制潜力，IC50 值在 2.46±0.008 和 312.79±0.06 μM 之间。在这一系列中，化合物 1、3、4、5、7、8 和 11 表现出优异的抑制潜力，IC50 值分别为 2.46±0.008、37.78±0.05、28.91±0.0、38.12±0.04、37.43±0.03、36.89±0.06 和 37.11±0.05 μM。其他所有化合物也表现出良好的酶抑制作用。通过分子对接证实了这些类似物的结合模式。
