Fourteen (hetero-)(arylidene)arylhydrazide derivatives (ABH1–ABH14) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound ABH5 most potently inhibited MAO-B with an IC₅₀ value of 0.025 ± 0.0019 μM; ABH2 and ABH3 exhibited high IC₅₀ values as well. Most of the compounds weakly inhibited MAO-A, except ABH5 (IC₅₀ = 3.31 ± 0.41 μM). Among the active compounds, ABH2 showed the highest selectivity index (SI) of 174 for MAO-B, followed by ABH5 (SI = 132). ABH3 and ABH5 effectively inhibited AChE with IC₅₀ values of 15.7 ± 6.52 and 16.5 ± 7.29 μM, respectively, whereas the other compounds were weak inhibitors of AChE. ABH5 was shown to be a reversible competitive inhibitor for MAO-A and MAO-B with K_i 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.

中文翻译：

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(杂-)(亚芳基)芳基酰肼作为多靶点单胺氧化酶抑制剂

合成了十四种（杂-）（亚芳基）芳基酰肼衍生物（ABH1 - ABH14），并评估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ABH5最有效地抑制 MAO-B，IC ₅₀值为 0.025 ± 0.0019 μM；ABH2和ABH3也表现出高IC ₅₀值。除了ABH5 (IC ₅₀ = 3.31 ± 0.41 μM) ，大多数化合物对 MAO-A 的抑制作用较弱。在活性化合物中，ABH2对 MAO-B 的选择性指数 (SI) 最高，为 174，其次是ABH5 (SI = 132)。ABH3和ABH5有效抑制 AChE，IC ₅₀值分别为 15.7 ± 6.52 和 16.5 ± 7.29 μM，而其他化合物是 AChE 的弱抑制剂。ABH5被证明是 MAO-A 和 MAO-B 的可逆竞争性抑制剂，K _i值分别为 0.96 ± 0.19 和 0.024 ± 0.0077 μM，表明该分子可被视为进一步开发为多靶点的有趣候选物与神经退行性疾病相关的抑制剂。