Show simple item record

dc.contributor.authorNel, Magdalena S.
dc.contributor.authorPetzer, Anél
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorLegoabe, Lesetja J.
dc.date.accessioned2016-10-31T08:38:01Z
dc.date.available2016-10-31T08:38:01Z
dc.date.issued2016
dc.identifier.citationNel, M.S. et al. 2016. 2-Heteroarylidene-1-indanone derivatives as inhibitors of monoamine oxidase. Bioorganic chemistry, 69:20-28. [https://doi.org/10.1016/j.bioorg.2016.09.004]en_US
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/19234
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2016.09.004
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0045206816302024
dc.description.abstractIn the present study a series of fifteen 2-heteroarylidene-1-indanone derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. These compounds are structurally related to series of heterocyclic chalcone derivatives which have previously been shown to act as MAO-B specific inhibitors. The results document that the 2-heteroarylidene-1-indanones are in vitro inhibitors of MAO-B, displaying IC50 values of 0.0044–1.53 μM. Although with lower potencies, the derivatives also inhibit the MAO-A isoform with IC50 values as low as 0.061 μM. An analysis of the structure-activity relationships for MAO-B inhibition indicates that substitution with the methoxy group on the A-ring leads to a significant enhancement in MAO-B inhibition compared to the unsubstituted homologues while the effect of the heteroaromatic substituent on activity, in decreasing order is: 5-bromo-2-furan > 5-methyl-2-furan > 2-pyridine ≈ 2-thiophene > cyclohexyl > 3-pyridine ≈ 2-furan. It may therefore be concluded that 2-heteroarylidene-1-indanone derivatives are promising leads for the design of MAO inhibitors for the treatment of Parkinson’s disease and possibly other neurodegenerative disordersen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectIndanoneen_US
dc.subjectMonoamine oxidaseen_US
dc.subjectMAOen_US
dc.subjectInhibitionen_US
dc.subjectChalconeen_US
dc.subjectSARen_US
dc.subjectHeterocyclicen_US
dc.title2-Heteroarylidene-1-indanone derivatives as inhibitors of monoamine oxidaseen_US
dc.typeArticleen_US
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan
dc.contributor.researchID22683178 - Nel, Magdalena Salomina


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record