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Molecules 2016, 21(5), 634; doi:10.3390/molecules21050634

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

1
Laboratory of Applied Chemistry, Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax, B.P. 802, Sfax 3000, Tunisia
2
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
3
Laboratory of Cell Toxicology, EA 4267, University of Bourgogne Franche-Comté, 19 rue Ambroise Paré, Besançon Cedex 25030, France
4
Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, Ljubljana 1000, Slovenia
5
Department of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9 Street, Krakow 30-688, Poland
6
Laboratory of Medicinal Chemistry (IQOG, CSIC) C/Juan de la Cierva 3, Madrid 28006, Spain
7
Biomedical Research Center, University Hospital Hradec Kralove, 500 05 Hradec Králove, Czech Republic
Present Address: Centre de Recherche de Gif-sur-Yvette, Institut de Chimie des Substances Naturelles, UPR 2301, CNRS, Avenue de la Terrasse, Gif-sur-Yvette 91198, France.
*
Authors to whom correspondence should be addressed.
Academic Editors: Michael Decker and Diego Muñoz-Torrero
Received: 18 February 2016 / Revised: 19 April 2016 / Accepted: 4 May 2016 / Published: 14 May 2016
(This article belongs to the Special Issue Molecules against Alzheimer)
View Full-Text   |   Download PDF [1417 KB, uploaded 14 May 2016]   |  

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. View Full-Text
Keywords: Alzheimer’s disease; quinazolinones; multicomponent reactions; multitarget-directed ligands; antioxidants; cholinesterase inhibitors; hepatotoxicity Alzheimer’s disease; quinazolinones; multicomponent reactions; multitarget-directed ligands; antioxidants; cholinesterase inhibitors; hepatotoxicity
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MDPI and ACS Style

Dgachi, Y.; Bautista-Aguilera, O.M.; Benchekroun, M.; Martin, H.; Bonet, A.; Knez, D.; Godyń, J.; Malawska, B.; Gobec, S.; Chioua, M.; Janockova, J.; Soukup, O.; Chabchoub, F.; Marco-Contelles, J.; Ismaili, L. Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease. Molecules 2016, 21, 634.

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