New Melatonin鈥?i>N,N-Dibenzyl(N-methyl)amine Hybrids: Potent Neurogenic Agents with Antioxidant, Cholinergic, and Neuroprotective Properties as Innovative Drugs for Alzheimer鈥檚 Disea
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- 作者：Beatriz L贸pez-Iglesias ; Concepci贸n P茅rez ; Jos茅 A. Morales-Garc铆a ; Sandra Alonso-Gil ; Ana P茅rez-Castillo ; Alejandro Romero ; Manuela G. L贸pez ; Mercedes Villarroya ; Santiago Conde ; Mar铆a Isabel Rodr铆guez-Franco
- 刊名：Journal of Medicinal Chemistry
- 出版年：2014
- 出版时间：May 8, 2014
- 年：2014
- 卷：57
- 期：9
- 页码：3773-3785
- 全文大小：472K
- 年卷期：v.57,no.9(May 8, 2014)
- ISSN：1520-4804
文摘
Here, we describe a new family of melatonin鈥?i>N,N-dibenzyl(N-methyl)amine hybrids that show a balanced multifunctional profile covering neurogenic, antioxidant, cholinergic, and neuroprotective properties at low-micromolar 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 尾-amyloid aggregation promoted by AChE. In addition, they show low cell toxicity and can penetrate into the CNS. This multifunctional profile highlights these melatonin鈥?i>N,N-dibenzyl(N-methyl)amine hybrids as useful prototypes in the research of innovative drugs for Alzheimer鈥檚 disease.