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A new guanylhydrazone derivative as a potential acetylcholinesterase inhibitor for Alzheimer's disease: synthesis, molecular docking, biological evaluation and kinetic studies by nuclear magnetic resonance

机译:一种新型的胍hydr衍生物,可作为阿尔茨海默氏病的潜在乙酰胆碱酯酶抑制剂:合成,分子对接,生物学评估和核磁共振动力学研究

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The development of pharmacological agents for the treatment of Alzheimer's Disease (AD) is very relevant since this is the most common type of dementia. The inhibition of acetylcholinesterase (AChE) is important to increase the low levels of acetylcholine (ACh) neurotransmitter observed in sick people, which is associated with the memory loss. In this work, a new guanylhydrazone was designed and synthesized as an AChE inhibitor. This new compound was compared to tacrine and other guanylhydrazones. All of them were studied by molecular docking and tested in vitro as AChE inhibitors by Ellman's test and Fig-NMR method. A high inhibition of AChE by the new compound was observed, showing that this compound has great potential for the treatment of AD.
机译:由于这是痴呆症的最常见类型,因此开发用于治疗阿尔茨海默氏病(AD)的药物非常重要。抑制乙酰胆碱酯酶(AChE)对于增加在患者中观察到的低水平的乙酰胆碱(ACh)神经递质很重要,这与记忆力丧失有关。在这项工作中,设计并合成了一种新的胍hydr作为AChE抑制剂。将该新化合物与他克林和其他胍基compared进行了比较。所有这些都通过分子对接进行了研究,并通过Ellman检验和Fig-NMR方法在体外体外了作为AChE抑制剂的测试。观察到新化合物对AChE的高度抑制作用,表明该化合物具有治疗AD的巨大潜力。

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