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Synthesis And Biological Evaluation Of Benzochromenopyrimidinones As Cholinesterase Inhibitors And Potent Antioxidant, Non-Hepatotoxic Agents For Alzheimer'S Disease

Youssef Dgachi,Oscar M. Bautista-Aguilera,Mohamed Benchekroun,Helene Martin,Alexandre Bonet,Damijan Knez,Justyna Godyn,Barbara Malawska,Stanislav Gobec,Mourad Chioua,Jana Janockova,Ondrej Soukup,Fakher Chabchoub,Jose Marco-Contelles,Lhassane Ismaili

MOLECULES（2016）

Cited 23|Views11
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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 mu M), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.
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Key words
Alzheimer's disease,quinazolinones,multicomponent reactions,multitarget-directed ligands,antioxidants,cholinesterase inhibitors,hepatotoxicity
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