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Publication Type : Journal Article
Publisher : ChemMedChem
Source : ChemMedChem, Volume 11, Issue 24, p.2649-2655 (2016)
Keywords : Catalytic Domain, Chalcones, Chlorine, enzyme activation, Hep G2 Cells, Humans, Methane, Molecular Docking Simulation, Monoamine oxidase, Monoamine Oxidase Inhibitors
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2016
Abstract : Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series of twenty chalcones containing electron-donating and electron-withdrawing substituents were synthesized. All compounds were found to be competitive, selective, and reversible inhibitors of hMAO-B except (2E)-1-(4-methylphenyl)-3-(4-nitrophenyl)prop-2-en-1-one (P7) and (2E)-1-(4-chlorophenyl)-3-(4-nitrophenyl)prop-2-en-1-one (P17), which were found to be selective inhibitors of hMAO-A. The most potent hMAO-B inhibitor, (2E)-1-(4-chlorophenyl)-3-(4-ethylphenyl)prop-2-en-1-one (P16), showed a K value of 0.11±0.01 μm. Molecular docking simulations were carried out to identify the hypothetical binding mode for the most potent compounds in the active sites of hMAO-A and B. The ability of the compounds to cross the blood-brain barrier was assessed by parallel artificial membrane permeability assay (PAMPA). Additionally, the most potent hMAO-B inhibitor P16 showed no toxicity in cultured hepatic cells at concentrations of 5 and 25 μm.
Cite this Research Publication : Bijo Mathew, Ucar, G., Mathew, G. Elizabeth, Mathew, S., Purapurath, P. Kalatharak, Moolayil, F., Mohan, S., and Gupta, S. Varghese, “Monoamine Oxidase Inhibitory Activity: Methyl- versus Chlorochalcone Derivatives.”, ChemMedChem, vol. 11, no. 24, pp. 2649-2655, 2016.