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首页> 外文期刊>Journal of Medicinal Chemistry >New Melatonin?N,N?Dibenzyl(N?methyl)amine Hybrids: Potent Neurogenic Agents with Antioxidant, Cholinergic, and Neuroprotective Properties as Innovative Drugs for Alzheimer’s Disease
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New Melatonin?N,N?Dibenzyl(N?methyl)amine Hybrids: Potent Neurogenic Agents with Antioxidant, Cholinergic, and Neuroprotective Properties as Innovative Drugs for Alzheimer’s Disease

机译:新型褪黑素?N,N?二苄基(N?甲基)胺杂化物:具有抗氧化,胆碱能和神经保护特性的有效神经原性药物,可作为阿尔茨海默氏病的创新药物

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摘要

Here, we describe a new family of melatonin?N,N-dibenzyl(Nmethyl) amine hybrids that show a balanced multifunctional profile covering neurogenic, antioxidant, cholinergic, and neuroprotective properties at lowmicromolar concentrations. They promote maturation of neural stem cells into a neuronal phenotype and thus they could contribute to CNS repair. They also protect neural cells against mitochondrial oxidative stress, show antioxidant properties, and inhibit human acetylcholinesterase (AChE). Moreover, they displace propidium from the peripheral anionic site of AChE, preventing the β- amyloid aggregation promoted by AChE. In addition, they show low cell toxicity and can penetrate into the CNS. This multifunctional profile highlights these melatonin?N,N-dibenzyl(N-methyl)amine hybrids as useful prototypes in the research of innovative drugs for Alzheimer’s disease.
机译:在这里,我们描述了褪黑素?N,N-二苄基(N甲基)胺杂化物的一个新家族,该杂种在低微摩尔浓度下显示出平衡的多功能特性,涵盖神经原性,抗氧化剂,胆碱能和神经保护特性。它们促进神经干细胞成熟为神经元表型,因此它们可能有助于中枢神经系统的修复。它们还保护神经细胞免受线粒体氧化应激,显示抗氧化性能,并抑制人乙酰胆碱酯酶(AChE)。此外,它们从AChE的周围阴离子位点置换了丙锭,从而防止了AChE促进的β-淀粉样蛋白聚集。此外,它们显示出低细胞毒性,并且可以渗透到CNS中。这种多功能的特点突出了这些褪黑素?

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