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Título: | Synthesis of new ferulic/lipoic/comenic acid-melatonin hybrids as antioxidants and Nrf2 activators via Ugi reaction |
Autor: | Pachón-Angona, I.; Martin, Helene; Chhor, S.; Oset-Gasque, María Jesús; Refouvelet, B.; Marco-Contelles, José CSIC ORCID; Ismaili, L. | Fecha de publicación: | 2019 | Citación: | Future Medicinal Chemistry 11: 3097-3108 (2019) | Resumen: | Aim: Oxidative stress has been implicated in the pathogenesis of many neurodegenerative diseases, and particularly in Alzheimer's disease. Results: This work describes the Ugi multicomponent synthesis, antioxidant power and Nrf2 pathway induction in antioxidant response element cells of (E)-N-(2-((2-(1H-indol-3-yl)ethyl)amino)-2-oxoethyl)-N-(2-(5-(benzyloxy)-1H-indol-3-yl)ethyl)-3-(4-hydroxy-3-methoxyphenyl)acryl amides 8a-d, N-(2-((2-(1H-indol-3-yl)ethyl)amino)-2-oxoethyl)-N-(2-(5-(benzyloxy)-1H-indol-3-yl)ethyl)-5-(1,2-dithiolan-3-yl)pentanamides 8e-h and N-(2-((2-(1H-indol-3-yl)ethyl)amino)-2-oxoethyl)-N-(2-(5-(benzyloxy)-1H-indol-3-yl)ethyl)-5-hydroxy-4-oxo-4H-pyran-2-carboxamides 8i,j. Conclusion: We have identified compounds 8e and 8g, showing a potent antioxidant capacity, a remarkable neuroprotective effect against the cell death induced by HO in SH-SY5Y cells, and a performing activation of the Nrf2 signaling pathway, as very interesting new antioxidant agents for pathologies that curse with oxidative stress. | Versión del editor: | http://dx.doi.org/10.4155/fmc-2019-0191 | URI: | http://hdl.handle.net/10261/203258 | DOI: | 10.4155/fmc-2019-0191 | Identificadores: | doi: 10.4155/fmc-2019-0191 issn: 1756-8919 e-issn: 1756-8927 |
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