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

Y. Dgachi, O. Sokolov, V. Luzet, J. Godyń, D. Panek, A. Bonet, H. Martin, I. Iriepa, I. Moraleda, C. García-Iriepa, J. Janockova, L. Richert, O. Soukup, B. Malawska, F. Chabchoub, J. Marco-Contelles, L. Ismaili,

. 2017 ; 126 (-) : 576-589. [pub] 20161123

Jazyk angličtina Země Francie

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc17013359

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.

Citace poskytuje Crossref.org

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$a Herein we report an efficient two step synthesis and biological assessment of 12 racemic tetrahydropyranodiquinolin-8-amines derivatives as antioxidant, cholinesterase inhibitors and non-hepatotoxic agents. Based on the results of the primary screening, we identified 7-(3-methoxyphenyl)-9,10,11,12-tetrahydro-7H-pyrano[2,3-b:5,6-h']diquinolin-8-amine (2h) as a particularly interesting non-hepatotoxic compound that shows moderate antioxidant activity (1.83 equiv Trolox in the ORAC assay), a non competitive inhibition of hAChE (IC50 = 0.75 ± 0.01 μM), and brain permeable as determined by the PAMPA-Blood Brain Barrier assay.
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$a Luzet, Vincent $u Laboratoire de Chimie Organique et Thérapeutique, Neurosciences intégratives et cliniques, EA 481, Univ. Franche-Comté, Univ. Bourgogne Franche-Comté, UFR SMP, 19, rue Ambroise Paré, F-25000 Besançon, France.
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$a Godyń, Justyna $u Department of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9 Street, 30-688 Krakow, Poland.
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$a Iriepa, Isabel $u Department of Organic Chemistry and Inorganic Chemistry, School of Biology, Enviromental Sciences and Chemistry, University Alcala, Ctra. Barcelona, Km. 33.6, 28871 Alcala de Henares, Spain.
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$a Moraleda, Ignacio $u Department of Organic Chemistry and Inorganic Chemistry, School of Biology, Enviromental Sciences and Chemistry, University Alcala, Ctra. Barcelona, Km. 33.6, 28871 Alcala de Henares, Spain.
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$a García-Iriepa, Cristina $u Department of Analytical Chemistry, Physical Chemistry, and Chemical Engineering, School of Biology, Enviromental Sciences and Chemistry, University Alcala, Ctra. Barcelona, Km. 33.6, 28871 Alcala de Henares, Spain.
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$a Soukup, Ondrej $u Biomedical Research Center, University Hospital Hradec Kralove, Czechia.
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$a Marco-Contelles, José $u Laboratory of Medicinal Chemistry (IQOG, CSIC), C/ Juan de la Cierva 3, 28006 Madrid, Spain. Electronic address: iqoc21@iqog.csic.es.
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