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    3-Coumaranone derivatives as inhibitors of monoamine oxidase

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    3-Coumaranone derivatives.pdf (543.0Kb)
    Date
    2015
    Author
    Van Dyk, Adriaan S.
    Petzer, Jacobus P.
    Petzer, Anél
    Legoabe, Lesetja J.
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    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
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    http://hdl.handle.net/10394/18360
    https://www.dovepress.com/3-coumaranone-derivatives-as-inhibitors-of-monoamine-oxidase-peer-reviewed-article-DDDT
    https://doi.org/10.2147/DDDT.S89961
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