Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9967-9973
2016
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Details
- Autor(en) / Beteiligte
- Titel
- 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
- Ist Teil von
- Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9967-9973
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2016
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/acs.jmedchem.6b01178Titel-ID: cdi_hal_primary_oai_HAL_hal_01460668v1
- Format
- –
- Schlagworte
- Alzheimer Disease - drug therapy, Alzheimer Disease - metabolism, Antioxidants - chemical synthesis, Antioxidants - chemistry, Antioxidants - pharmacology, Cell Death - drug effects, Cell Survival - drug effects, Chemical Sciences, Cholinesterase Inhibitors - chemical synthesis, Cholinesterase Inhibitors - chemistry, Cholinesterase Inhibitors - pharmacology, Cholinesterases - metabolism, Coumaric Acids - chemical synthesis, Coumaric Acids - chemistry, Coumaric Acids - pharmacology, Dose-Response Relationship, Drug, Hep G2 Cells, Humans, Melatonin - chemical synthesis, Melatonin - chemistry, Melatonin - pharmacology, Molecular Structure, NF-E2-Related Factor 2 - agonists, NF-E2-Related Factor 2 - metabolism, Structure-Activity Relationship