dc.contributor.author | Legoabe, Lesetja J. | |
dc.contributor.author | Petzer, Anél | |
dc.contributor.author | Petzer, Jacobus P. | |
dc.date.accessioned | 2014-01-09T08:03:13Z | |
dc.date.available | 2014-01-09T08:03:13Z | |
dc.date.issued | 2012 | |
dc.identifier.citation | Legoabe, L.J. et al. 2012. Selected chromone derivatives as inhibitors of monoamine oxidase. Bioorganic & medicinal chemistry letters, 22(17):5480-5484. [https://doi.org/10.1016/j.bmcl.2012.07.025] | en_US |
dc.identifier.issn | 0960-894X | |
dc.identifier.issn | 1464-3405 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/9892 | |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0960894X1200892X | |
dc.identifier.uri | https://doi.org/10.1016/j.bmcl.2012.07.025 | |
dc.description.abstract | A previous study has shown that a series of C6-benzyloxy substituted chromones exhibit high binding affinities for human monoamine oxidase (MAO) B. In an attempt to discover additional chromones with potent and selective MAO-B inhibitory potencies and to further examine the structure-activity relationships of MAO-B inhibition by chromones, the series was expanded with homologues containing polar functional groups on C3 of the chromone ring. The results demonstrate that 6-[(3-bromobenzyl)oxy]chromones containing acidic and aldehydic functional groups on C3 act as potent reversible MAO-B inhibitors with IC50 values of 2.8 and 3.7 nM, respectively. Interestingly, a 2-hydroxy-2,3-dihydro-1-benzopyran-4-one derivative as well as open-ring 2-acetylphenol analogues of the chromones also were potent MAO-B inhibitors with IC50 values ranging from 4 to 11 nM. Chromone derivatives containing the benzyloxy substituent on C5 of the chromone ring, however, exhibit MAO-B inhibition potencies that are several orders of magnitude weaker. High potency inhibitors of MAO-B may find application in the therapy of neurodegenerative disorders such as Parkinson’s disease. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | Chromone | en_US |
dc.subject | Benzopyran-4-one | en_US |
dc.subject | Monoamine oxidase | en_US |
dc.subject | MAO-B | en_US |
dc.subject | Reversible inhibition | en_US |
dc.subject | Structure-activity relationships | en_US |
dc.title | Selected chromone derivatives as inhibitors of monoamine oxidase | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 12264954 - Petzer, Anél | |
dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
dc.contributor.researchID | 12902608 - Legoabe, Lesetja Jan | |