Dual-target anti-Alzheimer’s disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activity

MAO-B leads to an increase in the levels of hydrogen peroxide and oxidative free radicals, which contribute to the aetiology of the AD. Thus, both iron ion chelators and MAO-B inhibitors can be used to treat AD. Taking the coumarin derivatives and hydroxypyridinones as the lead compounds, a series o...

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Detalles Bibliográficos
Autores principales: Mi, Zhisheng, Gan, Bing, Yu, Sihang, Guo, Jianan, Zhang, Changjun, Jiang, Xiaoying, Zhou, Tao, Su, Jing, Bai, Renren, Xie, Yuanyuan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6713216/
https://www.ncbi.nlm.nih.gov/pubmed/31416364
http://dx.doi.org/10.1080/14756366.2019.1634703
Descripción
Sumario:MAO-B leads to an increase in the levels of hydrogen peroxide and oxidative free radicals, which contribute to the aetiology of the AD. Thus, both iron ion chelators and MAO-B inhibitors can be used to treat AD. Taking the coumarin derivatives and hydroxypyridinones as the lead compounds, a series of dual-target hybrids were designed and synthesised by Click Chemistry. The compounds were biologically evaluated for their iron ion chelating and MAO-B inhibitory activity. Most of the compounds displayed excellent iron ion chelating activity and moderate to good anti-MAO-B activity. Compounds 27b and 27j exhibited the most potent MAO-B inhibitory activity, with IC(50) values of 0.68 and 0.86 μM, respectively. In summary, these dual-target compounds have the potential anti-AD activity.

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