| Literature DB >> 27736061 |
Mohamed Benchekroun1, Alejandro Romero2, Javier Egea3,4, Rafael León3,4, Patrycja Michalska3,4, Izaskun Buendía3,4, María Luisa Jimeno5, Daniel Jun6, Jana Janockova7, Vendula Sepsova6, Ondrej Soukup7, Oscar M Bautista-Aguilera1, Bernard Refouvelet1, Olivier Ouari8, José Marco-Contelles9, Lhassane Ismaili1.
Abstract
Novel multifunctional tacrines for Alzheimer's disease were obtained by Ugi-reaction between ferulic (or lipoic acid), a melatonin-like isocyanide, formaldehyde, and tacrine derivatives, according to the antioxidant additive approach in order to modulate the oxidative stress as therapeutic strategy. Compound 5c has been identified as a promising permeable agent showing excellent antioxidant properties, strong cholinesterase inhibitory activity, less hepatotoxicity than tacrine, and the best neuroprotective capacity, being able to significantly activate the Nrf2 transcriptional pathway.Entities:
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Year: 2016 PMID： 27736061 DOI： 10.1021/acs.jmedchem.6b01178
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446