Our goal was the evaluation of a series of N-1,2,3-triazole-isatin derivatives for multi-target activity which included cholinesterase (ChE) inhibition and β-amyloid (Aβ) peptide anti-aggregation. The compounds have shown considerable promise as butyrylcholinesterase (BuChE) inhibitors. Although the inhibition of eel acetylcholinesterase (eeAChE) was weak, the inhibitions against equine BuChE (eqBuChE) and human BuChE (hBuChE) were more significant with a best inhibition against eqBuChE of 0.46 μM. In some cases, these molecules gave better inhibitions for hBuChE than eqBuChE. For greater insights into their mode of action, molecular docking studies were carried out, followed by STD-NMR validation. In addition, some of these compounds showed weak Aβ anti-aggregation activity. Hepatotoxicity studies showed that they were non-hepatoxic and neurotoxicity studies using neurite outgrowth experiments led to the conclusion that these compounds are only weakly neurotoxic.

中文翻译：

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用于胆碱酯酶和β-淀粉样蛋白聚集抑制的N-1,2,3-三唑-isatin衍生物：全面的生物测定研究。

我们的目标是评估一系列N-1,2,3-三唑-isatin衍生物的多目标活性，其中包括胆碱酯酶（ChE）抑制和β-淀粉样蛋白（Aβ）肽抗聚集。该化合物作为丁酰胆碱酯酶（BuChE）抑制剂已显示出可观的前景。尽管对鳗鱼乙酰胆碱酯酶（eeAChE）的抑制作用较弱，但对马BuChE（eqBuChE）和人BuChE（hBuChE）的抑制作用更为显着，对eqBuChE的最佳抑制作用为0.46μM。在某些情况下，这些分子对hBuChE的抑制作用要强于eqBuChE。为了更深入地了解其作用方式，进行了分子对接研究，然后进行了STD-NMR验证。另外，这些化合物中的一些显示出弱的Aβ抗聚集活性。