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Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer's Disease

Y. Dgachi, OM. Bautista-Aguilera, M. Benchekroun, H. Martin, A. Bonet, D. Knez, J. Godyń, B. Malawska, S. Gobec, M. Chioua, J. Janockova, O. Soukup, F. Chabchoub, J. Marco-Contelles, L. Ismaili,

. 2016 ; 21 (5) : . [pub] 20160514

Language English Country Switzerland

Document type Journal Article

Persistent link   https://www.medvik.cz/link/bmc17023979

We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC50 = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.

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$a Dgachi, Youssef $u Laboratory of Applied Chemistry, Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax, B.P. 802, Sfax 3000, Tunisia. youssefdgachi@gmail.com.
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$a Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer's Disease / $c Y. Dgachi, OM. Bautista-Aguilera, M. Benchekroun, H. Martin, A. Bonet, D. Knez, J. Godyń, B. Malawska, S. Gobec, M. Chioua, J. Janockova, O. Soukup, F. Chabchoub, J. Marco-Contelles, L. Ismaili,
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$a We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC50 = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.
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$a Bautista-Aguilera, Oscar M $u Laboratoire de Chimie Organique et Thérapeutique, Neurosciences Intégratives et Cliniques, EA 481, UFR SMP, Univ. Franche-Comté, Univ. Bourgogne Franche-Comté, 19, rue Ambroise Paré, Besançon F-25000, France. osmabaga@gmail.com.
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$a Benchekroun, Mohamed $u Laboratoire de Chimie Organique et Thérapeutique, Neurosciences Intégratives et Cliniques, EA 481, UFR SMP, Univ. Franche-Comté, Univ. Bourgogne Franche-Comté, 19, rue Ambroise Paré, Besançon F-25000, France. mohamed.benchekroun@outlook.com.
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$a Martin, Hélène $u Laboratory of Cell Toxicology, EA 4267, University of Bourgogne Franche-Comté, 19 rue Ambroise Paré, Besançon Cedex 25030, France. helene.martin@univ-fcomte.fr.
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$a Bonet, Alexandre $u Laboratory of Cell Toxicology, EA 4267, University of Bourgogne Franche-Comté, 19 rue Ambroise Paré, Besançon Cedex 25030, France. alexandre.bonet@univ-fcomte.fr.
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$a Knez, Damijan $u Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, Ljubljana 1000, Slovenia. damijan.knez@ffa.uni-lj.si.
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$a Godyń, Justyna $u Department of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9 Street, Krakow 30-688, Poland. justyna.godyn@uj.edu.pl.
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$a Malawska, Barbara $u Department of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9 Street, Krakow 30-688, Poland. mfmalaws@cyf-kr.edu.pl.
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$a Gobec, Stanislav $u Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, Ljubljana 1000, Slovenia. stanislav.gobec@ffa.uni-lj.si.
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$a Chioua, Mourad $u Laboratory of Medicinal Chemistry (IQOG, CSIC) C/Juan de la Cierva 3, Madrid 28006, Spain. mchioua@gmail.com.
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$a Janockova, Jana $u Biomedical Research Center, University Hospital Hradec Kralove, 500 05 Hradec Králove, Czech Republic. jana.janockova@fnhk.cz.
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$a Soukup, Ondrej $u Biomedical Research Center, University Hospital Hradec Kralove, 500 05 Hradec Králove, Czech Republic. soukup.ondrej@fnhk.cz.
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$a Chabchoub, Fakher $u Laboratory of Applied Chemistry, Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax, B.P. 802, Sfax 3000, Tunisia. fakher.chabchoub@yahoo.fr.
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$a Marco-Contelles, José $u Laboratory of Medicinal Chemistry (IQOG, CSIC) C/Juan de la Cierva 3, Madrid 28006, Spain. iqoc21@iqog.csic.es.
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$a Ismaili, Lhassane $u Laboratoire de Chimie Organique et Thérapeutique, Neurosciences Intégratives et Cliniques, EA 481, UFR SMP, Univ. Franche-Comté, Univ. Bourgogne Franche-Comté, 19, rue Ambroise Paré, Besançon F-25000, France. lhassane.ismaili@univ-fcomte.fr.
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