Inhibition of monoamine oxidase by indole and benzofuran derivatives
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)
URI
http://hdl.handle.net/10394/5995https://www.sciencedirect.com/science/article/pii/S022352341000485X
https://doi.org/10.1016/j.ejmech.2010.07.005
Collections
- Faculty of Health Sciences [2386]