Department of Pharmaceutical Chemistry, Al-Shifa College of Pharmacy, Perinthalmanna-679322, Kerala, India.
Department of Pharmacy, and Research Institute of Life Pharmaceutical Sciences, Sunchon National University, Suncheon 57922, Republic of Korea.
ACS Comb Sci. 2020 Nov 9;22(11):592-599. doi: 10.1021/acscombsci.0c00136. Epub 2020 Oct 13.
Fourteen (hetero-)(arylidene)arylhydrazide derivatives (-) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound most potently inhibited MAO-B with an IC value of 0.025 ± 0.0019 μM; and exhibited high IC values as well. Most of the compounds weakly inhibited MAO-A, except (IC = 3.31 ± 0.41 μM). Among the active compounds, showed the highest selectivity index (SI) of 174 for MAO-B, followed by (SI = 132). and effectively inhibited AChE with IC values of 15.7 ± 6.52 and 16.5 ± 7.29 μM, respectively, whereas the other compounds were weak inhibitors of AChE. was shown to be a reversible competitive inhibitor for MAO-A and MAO-B with values of 0.96 ± 0.19 and 0.024 ± 0.0077 μM, respectively, suggesting that this molecule can be considered as an interesting candidate for further development as a multitarget inhibitor relating to neurodegenerative disorders.
合成了 14 种（杂）（芳亚基）芳肼衍生物，并评价了它们对单胺氧化酶（MAO）和乙酰胆碱酯酶（AChE）的抑制活性。化合物 对 MAO-B 的抑制活性最强，IC 值为 0.025±0.0019μM； 和 也表现出较高的 IC 值。除 （IC = 3.31±0.41μM）外，大多数化合物对 MAO-A 的抑制作用较弱。在活性化合物中， 对 MAO-B 的选择性指数（SI）最高为 174，其次是 （SI = 132）。 和 对 AChE 的抑制作用较强，IC 值分别为 15.7±6.52 和 16.5±7.29μM，而其他化合物对 AChE 的抑制作用较弱。 对 MAO-A 和 MAO-B 均为可逆竞争性抑制剂， 值分别为 0.96±0.19 和 0.024±0.0077μM，表明该分子可作为与神经退行性疾病相关的多靶标抑制剂的进一步开发的候选物。
