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

Keywords

• Alzheimer's disease
• quinazolinones
• multicomponent reactions
• multitarget-directed ligands
• antioxidants
• cholinesterase inhibitors
• hepatotoxicity