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dc.contributor.authorMarais, Lereze
dc.contributor.authorPetzer, Anél
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorLegoabe, Lesetja J.
dc.date.accessioned2019-06-04T13:53:45Z
dc.date.available2019-06-04T13:53:45Z
dc.date.issued2020
dc.identifier.citationMarais, L. et al. 2020. The monoamine oxidase inhibition properties of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives. Molecular diversity, 24:391-406. [https://doi.org/10.1007/s11030-019-09960-5]en_US
dc.identifier.issn1381-1991
dc.identifier.issn1573-501X (Online)
dc.identifier.urihttp://hdl.handle.net/10394/32503
dc.identifier.urihttps://link.springer.com/article/10.1007/s11030-019-09960-5
dc.identifier.urihttps://doi.org/10.1007/s11030-019-09960-5
dc.description.abstractQuinazolinone compounds are of interest in medicinal chemistry since they display a wide range of biological properties. In the present study, a series of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO). Some of these quinazolinones are structurally related to a series of 3,4-dihydro-2(1H)-quinolinone derivatives, which have previously been reported to act as specific inhibitors of MAO-B. The results document that, among 37 compounds synthesised, seven displayed IC50 values < 1 µM for the inhibition of MAO-B. The most potent MAO-A inhibitor exhibits an IC50 value of 7.43 µM while the most potent MAO-B inhibitor possesses an IC50 value of 0.269 µM. Good-potency MAO inhibition was only observed among C6-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives with N1-substitution yielding comparatively low-potency inhibition. MAO-B-specific inhibitors such as some of the quinazolinone compounds investigated here may act as leads for the design of therapies for neurodegenerative disorders such as Parkinson’s diseaseen_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.subjectMonoamine oxidaseen_US
dc.subjectMAOen_US
dc.subjectInhibitionen_US
dc.subjectReversibleen_US
dc.subjectQuinazolinoneen_US
dc.subjectNeurodegenerative disordersen_US
dc.titleThe monoamine oxidase inhibition properties of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivativesen_US
dc.typeArticleen_US
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan
dc.contributor.researchID22161333 - Marais, Lereze


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