Inhibition of monoamine oxidases by benzimidazole chalcone derivatives
نویسندگان
چکیده
Abstract Ten benzimidazole chalcone derivatives were synthesized, and their monoamine oxidase (MAO) inhibitory activity was evaluated. Most compounds showed higher against MAO-B than MAO-A. Compound BCH2 exhibited an IC 50 value of 0.80 μM, thereby showing the most potent inhibition amongst all. In addition, highest selectivity index (SI) with SI 44.11 compared to Among substituents, halogen group best inhibition, ortho -position B ring better para -site. comparison -substituents, increased in order, -Cl > -Br -F -H. found be a competitive inhibitor enzyme optimum kinetics, where K i 0.25 ± 0.014 μM. reversibility experiment, recovery pattern after similar that lazabemide. Thus, is potent, reversible, selective has been suggested as candidate for treatment neurological disorders.
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ژورنال
عنوان ژورنال: Applied Biological Chemistry
سال: 2023
ISSN: ['2468-0834', '2468-0842']
DOI: https://doi.org/10.1186/s13765-023-00795-1