Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy
Jazyk angličtina Země Francie Médium print-electronic
Typ dokumentu časopisecké články
PubMed
27918993
DOI
10.1016/j.ejmech.2016.11.050
PII: S0223-5234(16)30988-6
Knihovny.cz E-zdroje
- Klíčová slova
- Acetylcholinesterase inhibitors, Alzheimer's disease, Antioxidants, Brain blood barrier, Hepatotoxicity, Molecular modeling, Multifunctional agents,
- MeSH
- acetylcholinesterasa MeSH
- Alzheimerova nemoc farmakoterapie MeSH
- aminochinoliny chemická syntéza farmakologie MeSH
- antioxidancia chemie farmakologie MeSH
- cholinesterasové inhibitory chemie farmakologie MeSH
- GPI-vázané proteiny antagonisté a inhibitory MeSH
- hematoencefalická bariéra metabolismus MeSH
- lékové postižení jater MeSH
- lidé MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- ACHE protein, human MeSH Prohlížeč
- aminochinoliny MeSH
- antioxidancia MeSH
- cholinesterasové inhibitory MeSH
- GPI-vázané proteiny MeSH
Herein we report an efficient two step synthesis and biological assessment of 12 racemic tetrahydropyranodiquinolin-8-amines derivatives as antioxidant, cholinesterase inhibitors and non-hepatotoxic agents. Based on the results of the primary screening, we identified 7-(3-methoxyphenyl)-9,10,11,12-tetrahydro-7H-pyrano[2,3-b:5,6-h']diquinolin-8-amine (2h) as a particularly interesting non-hepatotoxic compound that shows moderate antioxidant activity (1.83 equiv Trolox in the ORAC assay), a non competitive inhibition of hAChE (IC50 = 0.75 ± 0.01 μM), and brain permeable as determined by the PAMPA-Blood Brain Barrier assay.
Biomedical Research Center University Hospital Hradec Kralove Czechia
Laboratory of Medicinal Chemistry C Juan de la Cierva 3 28006 Madrid Spain
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