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dc.contributor.authorRobinson, Sarel J.
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorPetzer, Anél
dc.contributor.authorBergh, Jacobus J.
dc.contributor.authorLourens, Anna C.U.
dc.date.accessioned2015-04-15T07:56:00Z
dc.date.available2015-04-15T07:56:00Z
dc.date.issued2013
dc.identifier.citationRobinson, S.J. et al. 2013. Selected furanochalcones as inhibitors of monoamine oxidase. Bioorganic & medicinal chemistry letters, 23(17):4985-4989. [https://doi.org/10.1016/j.bmcl.2013.06.050]en_US
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/13691
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0960894X13007713
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2013.06.050
dc.description.abstractThe validity of the chalcone scaffold for the design of inhibitors of monoamine oxidase has previously been illustrated. In a systematic attempt to investigate the effect of heterocyclic substitution on the monoamine oxidase inhibitory properties of this versatile scaffold, a series of furanochalcones were synthesized. The results demonstrate that these furan substituted phenylpropenones exhibited moderate to good inhibitory activities towards MAO-B, but showed weak or no inhibition of the MAO-A enzyme. The most active compound, 2E-3-(5-chlorofuran-2-yl)-1-(3-chlorophenyl)prop-2-en-1-one, exhibited an IC50 value of 0.174 lM for the inhibition of MAO-B and 28.6 lM for the inhibition of MAO-A. Interestingly, contrary to data previously reported for chalcones, these furan substituted derivatives acted as reversible inhibitors, while kinetic analysis revealed a competitive mode of bindingen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectChalconeen_US
dc.subjectmonoamine oxidaseen_US
dc.subjectMAO-Ben_US
dc.subjectReversible inhibitionen_US
dc.subjectCompetitiveen_US
dc.titleSelected furanochalcones as inhibitors of monoamine oxidaseen_US
dc.typeArticleen_US
dc.contributor.researchID20367414 - Robinson, Sarel Johannes
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID10057072 - Bergh, Jacobus Johannes
dc.contributor.researchID10948724 - Lourens, Anna Catharina U.


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