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

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

Content Provider	Scilit
Author	Dgachi, Youssef Sokolov, Olga Luzet, Vincent Godyń, Justyna Panek, Dawid Bonet, Alexandre Martin, Hélène Iriepa, Isabel Moraleda, Ignacio García-Iriepa, Cristina Janockova, Jana Richert, Lysiane Soukup, Ondrej Malawska, Barbara Chabchoub, Fakher Marco-Contelles, José Ismaili, Lhassane
Copyright Year	2017
Description	Journal: European Journal of Medicinal Chemistry 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 (IC = 0.75 ± 0.01 μM), and brain permeable as determined by the PAMPA-Blood Brain Barrier assay.
Related Links	https://digital.csic.es/bitstream/10261/149941/1/accesoRestringido.pdf
Ending Page	589
Page Count	14
Starting Page	576
ISSN	02235234
e-ISSN	17683254
DOI	10.1016/j.ejmech.2016.11.050
Journal	European Journal of Medicinal Chemistry
Volume Number	126
Language	English
Publisher	Elsevier BV
Publisher Date	2017-01-01
Access Restriction	Open
Subject Keyword	Journal: European Journal of Medicinal Chemistry Medicinal Chemistry Acetylcholinesterase Inhibitors Alzheimer's Disease Brain Blood Barrier Molecular Modeling Multifunctional Agents
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Medicine Drug Discovery Pharmacology

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