Quinolinyl-Thienyl Chalcones as Monoamine Oxidase Inhibitors and their In Silico Modeling Studies

Author(s): Sumera Zaib, Syed Umar Farooq Rizvi, Sana Aslam, Matloob Ahmad, Syed Mobasher Ali Abid, Mariya al-Rashida, Jamshed Iqbal

Journal Name: Medicinal Chemistry

Volume 11 , Issue 6 , 2015

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Graphical Abstract:


Mitochondrial enzymes monoamine oxidases were thought to be an emerging and useful therapeutic target for neurodegenerative disorders. Monoamine oxidases have two isoforms, A and B. MAO-A is related with metabolism of amine neurotransmitters in the brain whereas MAO-B is concerned with aging related neurodegenerative disorders. Therefore the identification, characterization and discovery of potent MAO-A and B inhibitors is very crucial in research. A series of quinolyl-thienyl chalcones were tested against MAO-A and B. Among the screened compounds, most of them revealed potent MAO-A and B inhibition. Compound 5i presented most potent MAO-A inhibition having IC50 values 0.047 µM, while 4l showed excellent inhibitory potency against MAO-B among all the tested compound having IC50 values 0.063 µM. Molecular modelling studies were performed against human MAO-A and MAO-B for the explanation of binding site interactions.

Keywords: Aging, molecular modelling, monoamine oxidase, neurodegenerative disease, quinolinyl-thienyl chalcones.

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Article Details

Year: 2015
Page: [580 - 589]
Pages: 10
DOI: 10.2174/1573406410666141226131252
Price: $65

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PDF: 29