2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease
Jazyk angličtina Země Francie Médium print-electronic
Typ dokumentu časopisecké články
PubMed
33360800
DOI
10.1016/j.ejmech.2020.113112
PII: S0223-5234(20)31084-9
Knihovny.cz E-zdroje
- Klíčová slova
- Alzheimer’s disease, Amyloid-beta, Antioxidant, Inflammation, Monoamine oxidase, Multi-target directed ligand, Naphthoquinone,
- MeSH
- Alzheimerova nemoc farmakoterapie MeSH
- lidé MeSH
- naftochinony farmakologie terapeutické užití MeSH
- racionální návrh léčiv MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- naftochinony MeSH
Alzheimer's disease is a progressive brain disorder with characteristic symptoms and several pathological hallmarks. The concept of "one drug, one target" has not generated any new drugs since 2004. The new era of drug development in the field of AD builds upon rationally designed multi-target directed ligands that can better address the complexity of AD. Herewith, we designed ten novel derivatives of 2-propargylamino-naphthoquinone. The biological evaluation of these compounds includes inhibition of monoamine oxidase A/B, inhibition of amyloid-beta aggregation, radical-scavenging, and metal-chelating properties. Some of the compounds possess low cytotoxicity profile with an anti-inflammatory ability in the lipopolysaccharide-stimulated cellular model. All these features warrant their further testing in the field of AD.
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