Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia; Faculty of Applied Science, UiTM Shah Alam, 40450 Shah Alam, Selangor D.E., Malaysia.
Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia; Faculty of Applied Science, UiTM Shah Alam, 40450 Shah Alam, Selangor D.E., Malaysia.
Bioorg Chem. 2017 Aug;73:121-127. doi: 10.1016/j.bioorg.2017.06.007. Epub 2017 Jun 19.
A series of twenty indole hydrazone analogs (1-21) were synthesized, characterized by different spectroscopic techniques such as H NMR and EI-MS, and screened for α-amylase inhibitory activity. All analogs showed a variable degree of α-amylase inhibition with IC values ranging between 1.66 and 2.65μM. Nine compounds that are 1 (2.23±0.01μM), 8 (2.44±0.12μM), 10 (1.92±0.12μM), 12 (2.49±0.17μM), 13 (1.66±0.09μM), 17 (2.25±0.1μM), 18 (1.87±0.25μM), 20 (1.83±0.63μM), and 19 (1.97±0.02μM) showed potent α-amylase inhibition when compared with the standard acarbose (1.05±0.29μM). Other analogs showed good to moderate α-amylase inhibition. The structure activity relationship is mainly focusing on difference of substituents on phenyl part. Molecular docking studies were carried out to understand the binding interaction of the most active compounds.
合成了一系列二十个吲哚腙类似物（1-21），通过不同的光谱技术（如 H NMR 和 EI-MS）进行了表征，并筛选了它们对α-淀粉酶抑制活性。所有类似物均表现出不同程度的α-淀粉酶抑制活性，IC 值范围在 1.66 至 2.65μM 之间。有 9 种化合物表现出较强的α-淀粉酶抑制活性，其中 1 号化合物（2.23±0.01μM）、8 号化合物（2.44±0.12μM）、10 号化合物（1.92±0.12μM）、12 号化合物（2.49±0.17μM）、13 号化合物（1.66±0.09μM）、17 号化合物（2.25±0.1μM）、18 号化合物（1.87±0.25μM）、20 号化合物（1.83±0.63μM）和 19 号化合物（1.97±0.02μM）的抑制活性与标准阿卡波糖（1.05±0.29μM）相比更为显著。其他类似物也表现出良好至中等程度的α-淀粉酶抑制活性。构效关系主要集中在苯环部分取代基的差异上。进行了分子对接研究以了解最活跃化合物的结合相互作用。
