This study fast synthesizes numerous functionalized pyridoxines using click chemistry and assayed in vitro as inhibitors of the acetylcholinesterase (AChE), butyrylcholinesterase, and two monoamine oxidase (MAO) isoforms, MAO-A and MAO-B. Most of the obtained compounds demonstrate good AChE and selective MAO-B inhibitory activities in the micromolar range, especially one compound, called 4k5 , exhibits excellent inhibitory performance against AChE (IC 50 = 0.0816 ± 0.075 μM) and MAO-B (IC 50 = 0.039 ± 0.003 μM). Finally, a docking study is carried out, demonstrating potential binding orientations and interactions of the compounds in terms of the AChE and MAO-B active sites.

中文翻译：

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“点击”组装来自吡哆醇衍生物的新型 AChE 和 MAO-B 双重抑制剂用于治疗阿尔茨海默病

这项研究使用点击化学快速合成了许多功能化的吡哆醇，并在体外作为乙酰胆碱酯酶 (AChE)、丁酰胆碱酯酶和两种单胺氧化酶 (MAO) 异构体 MAO-A 和 MAO-B 的抑制剂进行了测定。大多数获得的化合物在微摩尔范围内表现出良好的 AChE 和选择性 MAO-B 抑制活性，特别是一种称为 4k5 的化合物对 AChE (IC 50 = 0.0816 ± 0.075 μM) 和 MAO-B (IC 50 = 0.039±0.003μM）。最后，进行了对接研究，证明了化合物在 AChE 和 MAO-B 活性位点方面的潜在结合方向和相互作用。