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.
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