Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/149941
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Title

Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy

AuthorsDgachi, Youssef; Sokolov, O.; Luzet, V.; Godyn, J.; Panek, D.; Bonet, A.; Martin, H.; Iriepa, Isabel; Moraleda, I.; García-Iriepa, C.; Janockova, J.; Richert, L.; Soukup, O.; Malawska, B.; Chabchoub, Fakher; Marco-Contelles, José CSIC ORCID; Ismaili, L.
KeywordsMultifunctional agents
Molecular modeling
Brain blood barrier
Hepatotoxicity
Antioxidants
Acetylcholinesterase inhibitors
Alzheimer's disease
Issue Date2017
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 126: 576-589 (2017)
AbstractHerein 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 (IC = 0.75 ± 0.01 μM), and brain permeable as determined by the PAMPA-Blood Brain Barrier assay.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2016.11.050
URIhttp://hdl.handle.net/10261/149941
DOI10.1016/j.ejmech.2016.11.050
Identifiersdoi: 10.1016/j.ejmech.2016.11.050
issn: 0223-5234
e-issn: 1768-3254
Appears in Collections:(IQOG) Artículos




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