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.

Biomedical Research Center University Hospital Hradec Kralove 500 05 Hradec Králove Czech Republic

Department of Physicochemical Drug Analysis Jagiellonian University Medical College Medyczna 9 Street Krakow 30 688 Poland

Faculty of Pharmacy University of Ljubljana Aškerčeva 7 Ljubljana 1000 Slovenia

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

Laboratory of Applied Chemistry Heterocycles Lipids and Polymers Faculty of Sciences of Sfax University of Sfax B P 802 Sfax 3000 Tunisia

Laboratory of Cell Toxicology EA 4267 University of Bourgogne Franche Comté 19 rue Ambroise Paré Besançon Cedex 25030 France

Laboratory of Medicinal Chemistry C Juan de la Cierva 3 Madrid 28006 Spain

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Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer's disease therapy

Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer's disease therapy