Inhibition of monoamine oxidase by indole and benzofuran derivatives
| dc.contributor.author | Prins, Louis H.A. | |
| dc.contributor.author | Petzer, Jacobus P. | |
| dc.contributor.author | Malan, Sarel F. | |
| dc.contributor.researchID | 10199667 - Malan, Sarel Francois | |
| dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
| dc.contributor.researchID | 12256129 - Prins, Louis Hendrik Albertus | |
| dc.date.accessioned | 2012-02-29T09:49:49Z | |
| dc.date.available | 2012-02-29T09:49:49Z | |
| dc.date.issued | 2010 | en_US |
| dc.description.abstract | Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. A series of indole and benzofuran derivatives were synthesised and evaluated as inhibitors of the two MAO isoforms, MAO-A and MAO-B. In general, the derivatives were found to be selective MAO-B inhibitors with Ki values in the nanoMolar (nM) to microMolar (μM) concentration range. The most potent MAO-B inhibitor, 3,4-dichloro-N-(2-methyl-1H-indol-5-yl)benzamide, exhibited a Ki value of 0.03 μM and was 99 fold more selective for the B isoform. We conclude that these indole and benzofuran derivatives are promising reversible MAO-B inhibitors with a possible role in the treatment of neurodegenerative diseases such as Parkinson's disease (PD) | |
| dc.identifier.citation | Prins, L.H.A. et al. 2010. Inhibition of monoamine oxidase by indole and benzofuran derivatives. European journal of medicinal chemistry, 45(10):4458-4466. [https://doi.org/10.1016/j.ejmech.2010.07.005] | en_US |
| dc.identifier.issn | 0223-5234 | en_US |
| dc.identifier.issn | 1768-3254 | en_US |
| dc.identifier.uri | http://hdl.handle.net/10394/5995 | |
| dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S022352341000485X | |
| dc.identifier.uri | https://doi.org/10.1016/j.ejmech.2010.07.005 | |
| dc.language.iso | en | |
| dc.publisher | Elsevier | en_US |
| dc.subject | Monoamine oxidase (MAO) | |
| dc.subject | Indole derivatives | |
| dc.subject | Benzofuran derivatives | |
| dc.subject | Parkinson’s disease (PD) | |
| dc.subject | Molecular docking | |
| dc.subject | LigandFit | |
| dc.title | Inhibition of monoamine oxidase by indole and benzofuran derivatives | en_US |