Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer's Disease
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Titre | Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer's Disease |
Type de publication | Journal Article |
Year of Publication | 2016 |
Auteurs | Dgachi 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 |
Journal | MOLECULES |
Volume | 21 |
Pagination | 634 |
Date Published | MAY |
Type of Article | Article |
ISSN | 1420-3049 |
Mots-clés | Alzheimer'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. |
DOI | 10.3390/molecules21050634 |