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

SUBMITTER: Dgachi Y

PROVIDER: S-EPMC6273488 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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

Dgachi Youssef Y Bautista-Aguilera Oscar M OM Benchekroun Mohamed M Martin Hélène H Bonet Alexandre A Knez Damijan D Godyń Justyna J Malawska Barbara B Gobec Stanislav S Chioua Mourad M Janockova Jana J Soukup Ondrej O Chabchoub Fakher F Marco-Contelles José J Ismaili Lhassane L

Molecules (Basel, Switzerland) 20160514 5

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 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line. ...[more]

PMID: 27187348

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