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

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TitreSynthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer's Disease
Type de publicationJournal Article
Year of Publication2016
AuteursDgachi Y, Bautista-Aguilera OM, Benchekroun M, Martin H, Bonet A, Knez D, Godyn J, Malawska B, Gobec S, Chioua M, Janockova J, Soukup O, Chabchoub F, Marco-Contelles J, Ismaili L
JournalMOLECULES
Volume21
Pagination634
Date PublishedMAY
Type of ArticleArticle
ISSN1420-3049
Mots-clésAlzheimer's disease, antioxidants, cholinesterase inhibitors, Hepatotoxicity, multicomponent reactions, multitarget-directed ligands, quinazolinones
Résumé

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 mu M), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.

DOI10.3390/molecules21050634