Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer’s disease therapy

We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer’s disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC(50) = 1...

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Detalles Bibliográficos
Autores principales: Pachón-Angona, Irene, Refouvelet, Bernard, Andrýs, Rudolf, Martin, Helène, Luzet, Vincent, Iriepa, Isabel, Moraleda, Ignacio, Diez-Iriepa, Daniel, Oset-Gasque, María-Jesús, Marco-Contelles, José, Musilek, Kamil, Ismaili, Lhassane
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6366423/
https://www.ncbi.nlm.nih.gov/pubmed/30712420
http://dx.doi.org/10.1080/14756366.2018.1545766
Descripción
Sumario:We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer’s disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC(50) = 11.90 ± 0.05 nM), moderate hAChE (IC(50) = 1.73 ± 0.34 μM), hMAO A (IC(50) = 2.78 ± 0.12 μM), and MAO B (IC(50) = 21.29 ± 3.85 μM) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.

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