title: Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer's Disease.
abstract: 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.
authors.affiliation: 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.
authors.forename: Youssef
authors.initials: Y
authors.lastname: Dgachi
authors.affiliation: 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.
authors.forename: Oscar M
authors.initials: OM
authors.lastname: Bautista-Aguilera
authors.affiliation: 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.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Benchekroun
authors.affiliation: Laboratory of Cell Toxicology, EA 4267, University of Bourgogne Franche-Comté, 19 rue Ambroise Paré, Besançon Cedex 25030, France. helene.martin@univ-fcomte.fr.
authors.forename: Hélène
authors.initials: H
authors.lastname: Martin
authors.affiliation: Laboratory of Cell Toxicology, EA 4267, University of Bourgogne Franche-Comté, 19 rue Ambroise Paré, Besançon Cedex 25030, France. alexandre.bonet@univ-fcomte.fr.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Bonet
authors.affiliation: Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, Ljubljana 1000, Slovenia. damijan.knez@ffa.uni-lj.si.
authors.forename: Damijan
authors.initials: D
authors.lastname: Knez
authors.affiliation: Department of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9 Street, Krakow 30-688, Poland. justyna.godyn@uj.edu.pl.
authors.forename: Justyna
authors.initials: J
authors.lastname: Godyń
authors.affiliation: Department of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9 Street, Krakow 30-688, Poland. mfmalaws@cyf-kr.edu.pl.
authors.forename: Barbara
authors.initials: B
authors.lastname: Malawska
authors.affiliation: Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, Ljubljana 1000, Slovenia. stanislav.gobec@ffa.uni-lj.si.
authors.forename: Stanislav
authors.initials: S
authors.lastname: Gobec
authors.affiliation: Laboratory of Medicinal Chemistry (IQOG, CSIC) C/Juan de la Cierva 3, Madrid 28006, Spain. mchioua@gmail.com.
authors.forename: Mourad
authors.initials: M
authors.lastname: Chioua
authors.affiliation: Biomedical Research Center, University Hospital Hradec Kralove, 500 05 Hradec Králove, Czech Republic. jana.janockova@fnhk.cz.
authors.forename: Jana
authors.initials: J
authors.lastname: Janockova
authors.affiliation: Biomedical Research Center, University Hospital Hradec Kralove, 500 05 Hradec Králove, Czech Republic. soukup.ondrej@fnhk.cz.
authors.forename: Ondrej
authors.initials: O
authors.lastname: Soukup
authors.affiliation: 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.
authors.forename: Fakher
authors.initials: F
authors.lastname: Chabchoub
authors.affiliation: Laboratory of Medicinal Chemistry (IQOG, CSIC) C/Juan de la Cierva 3, Madrid 28006, Spain. iqoc21@iqog.csic.es.
authors.forename: José
authors.initials: J
authors.lastname: Marco-Contelles
authors.affiliation: 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.
authors.forename: Lhassane
authors.initials: L
authors.lastname: Ismaili
mesh_terms: D000544:Alzheimer Disease / Q000517:prevention & control*; D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008099:Liver / Q000187:drug effects; D013057:Spectrum Analysis
chemical_list: D000975:Antioxidants; D002800:Cholinesterase Inhibitors
keywords: Alzheimer’s disease; antioxidants; cholinesterase inhibitors; hepatotoxicity; multicomponent reactions; multitarget-directed ligands; quinazolinones