dc.contributor.author | Van Dyk, Adriaan S. | |
dc.contributor.author | Petzer, Jacobus P. | |
dc.contributor.author | Petzer, Anél | |
dc.contributor.author | Legoabe, Lesetja J. | |
dc.date.accessioned | 2016-08-22T13:13:37Z | |
dc.date.available | 2016-08-22T13:13:37Z | |
dc.date.issued | 2015 | |
dc.identifier.citation | Van Dyk, A.S. et al. 2015. 3-Coumaranone derivatives as inhibitors of monoamine oxidase. Drug design, development and therapy, 9:5479-5489. [https://doi.org/10.2147/DDDT.S89961] | en_US |
dc.identifier.issn | 1177-8881 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/18360 | |
dc.identifier.uri | https://www.dovepress.com/3-coumaranone-derivatives-as-inhibitors-of-monoamine-oxidase-peer-reviewed-article-DDDT | |
dc.identifier.uri | https://doi.org/10.2147/DDDT.S89961 | |
dc.description.abstract | The present study examines the monoamine oxidase (MAO) inhibitory properties of a series of 20 3-coumaranone [benzofuran-3(2H)-one] derivatives. The 3-coumaranone derivatives are structurally related to series of α-tetralone and 1-indanone derivatives, which have recently been shown to potently inhibit MAO, with selectivity for MAO-B (in preference to the MAO-A isoform). 3-Coumaranones are similarly found to selectively inhibit human MAO-B with half-maximal inhibitory concentration (IC50) values of 0.004–1.05 μM. Nine compounds exhibited IC50,0.05 μM for the inhibition of MAO-B. For the inhibition of human MAO-A, IC50 values ranged from 0.586 to .100 μM, with only one compound possessing an IC50,1 μM. For selected 3-coumaranone derivatives, it is established that MAO-A and MAO-B inhibition are reversible since dialysis of enzyme–inhibitor mixtures almost completely restores enzyme activity. On the basis of the selectivity profiles and potent action, it may be concluded that the 3-coumaranone derivatives are suitable leads for the development of selective MAO-B inhibitors as potential treatment for disorders such as Parkinson’s disease and Alzheimer’s disease | en_US |
dc.description.sponsorship | Medical Research Council and National Research Foundation of South Africa (grant specific unique reference numbers [UID] 96180 and 85642) | en_US |
dc.language.iso | en | en_US |
dc.publisher | Dove Press | en_US |
dc.subject | MAO | en_US |
dc.subject | Benzofuran-3(2H)-one | en_US |
dc.subject | Inhibition | en_US |
dc.subject | Reversible | en_US |
dc.subject | Competitive | en_US |
dc.subject | Parkinson’s disease | en_US |
dc.title | 3-Coumaranone derivatives as inhibitors of monoamine oxidase | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 10791469 - Van Dyk, Adriaan Sarel | |
dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
dc.contributor.researchID | 12264954 - Petzer, Anél | |
dc.contributor.researchID | 12902608 - Legoabe, Lesetja Jan | |