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.
J Med Chem
; 59(21): 9967-9973, 2016 11 10.
Article
em En
| MEDLINE
| ID: mdl-27736061
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.
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Base de dados:
MEDLINE
Assunto principal:
Inibidores da Colinesterase
/
Ácidos Cumáricos
/
Fator 2 Relacionado a NF-E2
/
Doença de Alzheimer
/
Melatonina
/
Antioxidantes
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article