dc.contributor.author | Nel, Magdalena S. | |
dc.contributor.author | Petzer, Anél | |
dc.contributor.author | Petzer, Jacobus P. | |
dc.contributor.author | Legoabe, Lesetja J. | |
dc.date.accessioned | 2016-10-31T08:48:17Z | |
dc.date.available | 2016-10-31T08:48:17Z | |
dc.date.issued | 2016 | |
dc.identifier.citation | Nel, M.S. et al. 2016. 2-Benzylidene-1-indanone derivatives as inhibitors of monoamine oxidase. Bioorganic & medicinal chemistry letters, 26(19):4599-4605. [https://doi.org/10.1016/j.bmcl.2016.08.067] | en_US |
dc.identifier.issn | 0960-894X | |
dc.identifier.issn | 1464-3405 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/19235 | |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0960894X16309015 | |
dc.identifier.uri | https://doi.org/10.1016/j.bmcl.2016.08.067 | |
dc.description.abstract | In the present study, a series of twenty-two 2-benzylidene-1-indanone derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. The 2-benzylidene-1-indanone derivatives are structurally related to a series of benzylideneindanone derivatives which has previously been found to be MAO-B inhibitors. This study finds that the 2-benzylidene-1-indanones are MAO-B specific inhibitors with IC50 values <2.74 μM. Among the compounds evaluated, twelve compounds exhibited IC50 < 0.1 μM and may be considered as high potency inhibitors. The 2-benzylidene-1-indanone derivatives also inhibited MAO-A with the most potent inhibition exhibited by 5g (IC50 = 0.131 μM). An analysis of the structure–activity relationships for MAO-B inhibition show that substitution on the A-ring with a 5-hydroxy group and on the B-ring with halogens and the methyl group yield high potency inhibition. It may therefore be concluded that 2-benzylidene-1-indanone analogues are promising leads for design of therapies for disorders such as Parkinson’s disease | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | Monoamine oxidase | en_US |
dc.subject | MAO | en_US |
dc.subject | Inhibition | en_US |
dc.subject | Reversible | en_US |
dc.subject | 2-Benzylidene-1-indanone | en_US |
dc.title | 2-Benzylidene-1-indanone derivatives as inhibitors of monoamine oxidase | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 12902608 - Legoabe, Lesetja Jan | |
dc.contributor.researchID | 12264954 - Petzer, Anél | |
dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
dc.contributor.researchID | 22683178 - Nel, Magdalena Salomina | |