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

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

Volume: 11 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Zaib Sumera, Rizvi Umar Farooq Syed, Aslam Sana, Ahmad Matloob, Ali Abid Mobasher Syed, al-Rashida Mariya and Iqbal Jamshed, Quinolinyl-Thienyl Chalcones as Monoamine Oxidase Inhibitors and their In Silico Modeling Studies, Medicinal Chemistry 2015; 11 (6) . https://dx.doi.org/10.2174/1573406410666141226131252