3-Coumaranone derivatives as inhibitors of monoamine oxidase

View/ Open
Date
2015Author
Van Dyk, Adriaan S.
Petzer, Jacobus P.
Petzer, Anél
Legoabe, Lesetja J.
Metadata
Show full item recordAbstract
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
URI
http://hdl.handle.net/10394/18360https://www.dovepress.com/3-coumaranone-derivatives-as-inhibitors-of-monoamine-oxidase-peer-reviewed-article-DDDT
https://doi.org/10.2147/DDDT.S89961
Collections
- Faculty of Health Sciences [2404]