Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC50 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC50 55.21±0.12 μM).

中文翻译：

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新型双结合位点胆碱酯酶抑制剂的设计和合成：采用计算机对接的体外抑制研究

胆碱酯酶 (ChE) 在调节胆碱能传递中起着至关重要的作用。ChE 的抑制被认为与增加大脑中乙酰胆碱水平有关，因此与阿尔茨海默病的治疗有关。我们设计并合成了一系列新型吲哚衍生物，并筛选了它们对乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BChE) 的抑制作用。大多数测试化合物表现出对 AChE 和 BChE 的抑制活性。其中4f和6e表现出最高的AChE抑制活性，IC50分别为91.21±0.06和68.52±0.04 μM。然而，化合物 5a 对 BChE 表现出最高的抑制活性（IC50 55.21±0.12 μM）。