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dc.contributor.authorLegoabe, Lesetja J.
dc.contributor.authorPetzer, Anél
dc.contributor.authorPetzer, Jacobus P.
dc.identifier.citationLegoabe, L.J. et al. 2012. Inhibition of monoamine oxidase by selected C6-substituted chromone derivatives. European journal of medicinal chemistry, 49:343-353. []en_US
dc.description.abstractChromone has been reported to be a useful scaffold for the design of monoamine oxidase (MAO) inhibitors. In an attempt to discover highly potent MAO inhibitors and to contribute to the known structureeactivity relationships (SAR) of MAO inhibition by chromones, in the present study, we have synthesized a series of chromone derivatives substituted at C6 with a variety of alkyloxy substituents, and evaluated the resulting compounds as inhibitors of recombinant human MAO-A and -B. The results document that the C6-substituted chromones are potent reversible MAO-B inhibitors with IC50 values in the low nM range (2e76 nM). The chromones were also found to bind reversibly to MAO-A, but with lower affinities compared to MAO-B. It may therefore be concluded that C6-substituted chromones are highly potent MAO-B selective inhibitors and promising lead compounds for the development of therapy for neurodegenerative disorders such as Parkinson’s disease. The results of this study are discussed with reference to possible binding orientations of a selected C6-substituted chromone in the active site cavities of MAO-A and -B.en_US
dc.subjectMonoamine oxidaseen_US
dc.subjectReversible inhibitionen_US
dc.subjectCompetitive inhibitionen_US
dc.subjectMolecular dockingen_US
dc.subjectStructure-activity relationshipen_US
dc.titleInhibition of monoamine oxidase by selected C6-substituted chromone derivativesen_US
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus

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