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

descriptionPublicationkeyboard_double_arrow_right Article , Other literature type 14 May 2016 English Publisher:MDPI AGJournal:Molecules, volume 21, page 634 (eissn: 1420-3049, Copyright policy )
Authors: Youssef Dgachi; Oscar Bautista-Aguilera; Mohamed Benchekroun; Hélène Martin; Alexandre Bonet; Damijan Knez; Justyna Godyń; +8 Authors

doi: 10.3390/molecules21050634

pmid: 27187348

pmc: PMC6273488

handle: 10261/149207 , 20.500.12556/RUL-130298

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.

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Keywords

570, hepatotoxicity, cholinesterase inhibitors, quinazolinones, 610, Organic chemistry, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, info:eu-repo/classification/udc/615.2:616.894, Article, Antioxidants, Inhibitory Concentration 50, QD241-441, Alzheimer Disease, Humans, multitarget-directed ligands, Alzheimer’s disease; quinazolinones; multicomponent reactions; multitarget-directed ligands; antioxidants; cholinesterase inhibitors; hepatotoxicity, RS0400, [CHIM.ORGA]Chemical Sciences/Organic chemistry, multicomponent reactions, Spectrum Analysis, Alzheimer's disease, Alzheimerjeva bolezen, antioxidants, Liver, Cholinesterase Inhibitors, Alzheimer’s disease

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