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Quinolinyl-Thienyl Chalcones as Monoamine Oxidase Inhibitors and their in Silico Modeling Studies
Mitochondrial enzymes, monoamine oxidases (MAO) are thought to be emerging and useful therapeutic target for neurodegenerative disorders. Monoamine oxidases have two isoforms, A and B. MAO-A is related to metabolism of amine neurotransmitters in the brain whereas MAO-B is concerned with aging related neurodegenerative disorders. Therefore, the identification, characterization and discovery of new and potent MAO-A and B inhibitors is crucial in advancing neurodegenerative therapeutic research. A series of quinolinyl-thienyl chalcones were tested against MAO-A and B and most of them revealed potent MAO-A and B inhibition. Compound 5i exhibited most potent MAO-A inhibition activity, having IC50 value of 0.047 muM, while 4l showed maximum inhibitory potency against MAO-B having IC50 value of 0.063 muM. Molecular modelling studies were performed against human MAO-A and MAOB to rationalize most probable binding site interactions.
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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem