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dc.contributor.authorVan Dyk, Adriaan S.
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorPetzer, Anél
dc.contributor.authorLegoabe, Lesetja J.
dc.date.accessioned2016-08-22T13:13:37Z
dc.date.available2016-08-22T13:13:37Z
dc.date.issued2015
dc.identifier.citationVan Dyk, A.S. et al. 2015. 3-Coumaranone derivatives as inhibitors of monoamine oxidase. Drug design, development and therapy, 9:5479-5489. [https://doi.org/10.2147/DDDT.S89961]en_US
dc.identifier.issn1177-8881 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/18360
dc.identifier.urihttps://www.dovepress.com/3-coumaranone-derivatives-as-inhibitors-of-monoamine-oxidase-peer-reviewed-article-DDDT
dc.identifier.urihttps://doi.org/10.2147/DDDT.S89961
dc.description.abstractThe present study examines the monoamine oxidase (MAO) inhibitory properties of a series of 20 3-coumaranone [benzofuran-3(2H)-one] derivatives. The 3-coumaranone derivatives are structurally related to series of α-tetralone and 1-indanone derivatives, which have recently been shown to potently inhibit MAO, with selectivity for MAO-B (in preference to the MAO-A isoform). 3-Coumaranones are similarly found to selectively inhibit human MAO-B with half-maximal inhibitory concentration (IC50) values of 0.004–1.05 μM. Nine compounds exhibited IC50,0.05 μM for the inhibition of MAO-B. For the inhibition of human MAO-A, IC50 values ranged from 0.586 to .100 μM, with only one compound possessing an IC50,1 μM. For selected 3-coumaranone derivatives, it is established that MAO-A and MAO-B inhibition are reversible since dialysis of enzyme–inhibitor mixtures almost completely restores enzyme activity. On the basis of the selectivity profiles and potent action, it may be concluded that the 3-coumaranone derivatives are suitable leads for the development of selective MAO-B inhibitors as potential treatment for disorders such as Parkinson’s disease and Alzheimer’s diseaseen_US
dc.description.sponsorshipMedical Research Council and National Research Foundation of South Africa (grant specific unique reference numbers [UID] 96180 and 85642)en_US
dc.language.isoenen_US
dc.publisherDove Pressen_US
dc.subjectMAOen_US
dc.subjectBenzofuran-3(2H)-oneen_US
dc.subjectInhibitionen_US
dc.subjectReversibleen_US
dc.subjectCompetitiveen_US
dc.subjectParkinson’s diseaseen_US
dc.title3-Coumaranone derivatives as inhibitors of monoamine oxidaseen_US
dc.typeArticleen_US
dc.contributor.researchID10791469 - Van Dyk, Adriaan Sarel
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan


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