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

Authors :
Dgachi, Youssef
Bautista-Aguilera, Oscar M.
Benchekroun, Mohamed
Martin, Hélène
Bonet, Alexandre
Knez, Damijan
Godyń, Justyna
Malawska, Barbara
Gobec, Stanislav
Chioua, Mourad
Janockova, Jana
Soukup, Ondrej
Chabchoub, Fakher
Marco-Contelles, José
Ismaili, Lhassane
Source :
Molecules; May2016, Vol. 21 Issue 5, p634-648, 15p, 2 Diagrams, 3 Charts, 1 Graph
Publication Year :
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 (IC<subscript>50</subscript> = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
14203049
Volume :
21
Issue :
5
Database :
Complementary Index
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
115440524
Full Text :
https://doi.org/10.3390/molecules21050634