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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,
Jazyk angličtina Země Spojené státy americké
Typ dokumentu časopisecké články
- MeSH
- Alzheimerova nemoc farmakoterapie metabolismus MeSH
- antioxidancia chemická syntéza chemie farmakologie MeSH
- buněčná smrt účinky léků MeSH
- buňky Hep G2 MeSH
- cholinesterasové inhibitory chemická syntéza chemie farmakologie MeSH
- cholinesterasy metabolismus MeSH
- faktor 2 související s NF-E2 agonisté metabolismus MeSH
- kyseliny kumarové chemická syntéza chemie farmakologie MeSH
- lidé MeSH
- melatonin chemická syntéza chemie farmakologie MeSH
- molekulární struktura MeSH
- viabilita buněk účinky léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články 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
Citace poskytuje Crossref.org
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