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dc.contributor.authorShalaby, Raed
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorPetzer, Anél
dc.contributor.authorAshraf, Usman M.
dc.contributor.authorAtari, Ealla
dc.date.accessioned2019-04-23T08:27:58Z
dc.date.available2019-04-23T08:27:58Z
dc.date.issued2019
dc.identifier.citationShalaby, R. et al. 2019. SAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogs. Journal of enzyme inhibition and medicinal chemistry, 34(1):863-876. [https://doi.org/10.1080/14756366.2019.1593158]en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/32266
dc.identifier.urihttps://www.tandfonline.com/doi/full/10.1080/14756366.2019.1593158
dc.identifier.urihttps://doi.org/10.1080/14756366.2019.1593158
dc.description.abstractThe present study describes the synthesis of a series of 22 chalcone analogs. These compounds were evaluated as potential human MAO-A and MAO-B inhibitors. The compounds showed varied selectivity against the two isoforms. The IC50 values were found to be in the micromolar to submicromolar range. The Ki values of compound 16 were determined to be 0.047 and 0.020 μM for the inhibition of MAO-A and MAO-B, respectively. Dialysis of enzyme-inhibitor mixtures indicated a reversible competitive mode of inhibition. Most of the synthesized chalcone analogs showed a better selectivity toward MAO-B. However, introducing of 2,4,6-trimethoxy substituents on ring B shifted the selectivity toward MAO-A. In addition, we investigated the molecular mechanism of MAO-B inhibition by selected chalcone analogs. Our results revealed that these selected chalcone analogs increased dopamine levels in the rat hepatoma (H4IIE) cells and decreased the relative mRNA expression of the MAO-B enzymeen_US
dc.language.isoenen_US
dc.publisherTaylor & Francisen_US
dc.subjectMonoamine oxidaseen_US
dc.subjectChalconeen_US
dc.subjectReversibilityen_US
dc.subjectDopamineen_US
dc.subjectmRNAen_US
dc.titleSAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogsen_US
dc.typeArticleen_US
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12264954 - Petzer, Anél


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