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The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators
M. Benchekroun, A. Romero, J. Egea, R. León, P. Michalska, I. Buendía, ML. Jimeno, D. Jun, J. Janockova, V. Sepsova, O. Soukup, OM. Bautista-Aguilera, B. Refouvelet, O. Ouari, J. Marco-Contelles, L. Ismaili,
Journal of medicinal chemistry.
2016 ;
59 (21) :
9967-9973.
[pub] 20161031
Language English Country United States
Document type Journal Article
Persistent link
https://www.medvik.cz/link/bmc17023558
- MeSH
- Alzheimer Disease drug therapy metabolism MeSH
- Antioxidants chemical synthesis chemistry pharmacology MeSH
- Cell Death drug effects MeSH
- Hep G2 Cells MeSH
- Cholinesterase Inhibitors chemical synthesis chemistry pharmacology MeSH
- Cholinesterases metabolism MeSH
- NF-E2-Related Factor 2 agonists metabolism MeSH
- Coumaric Acids chemical synthesis chemistry pharmacology MeSH
- Humans MeSH
- Melatonin chemical synthesis chemistry pharmacology MeSH
- Molecular Structure MeSH
- Cell Survival drug effects MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
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.
Centro Química Orgánica Lora Tamayo CSIC C Juan de la Cierva 3 E 28006 Madrid Spain
ICR UMR 7273 Aix Marseille University CNRS 13013 Marseille France
Laboratory of Medicinal Chemistry IQOG CSIC C Juan de la Cierva 3 E 28006 Madrid Spain
References provided by Crossref.org
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