Show simple item record

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.identifier.citationRobinson, S.J. et al. 2013. Selected furanochalcones as inhibitors of monoamine oxidase. Bioorganic & medicinal chemistry letters, 23(17):4985-4989. []en_US
dc.identifier.issn1464-3405 (Online)
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.subjectmonoamine oxidaseen_US
dc.subjectReversible inhibitionen_US
dc.titleSelected furanochalcones as inhibitors of monoamine oxidaseen_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.

Files in this item


There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record