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    Selected furanochalcones as inhibitors of monoamine oxidase

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    Date
    2013
    Author
    Robinson, Sarel J.
    Petzer, Jacobus P.
    Petzer, Anél
    Bergh, Jacobus J.
    Lourens, Anna C.U.
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    Abstract
    The validity of the chalcone scaffold for the design of inhibitors of monoamine oxidase has previously been illustrated. In a systematic attempt to investigate the effect of heterocyclic substitution on the monoamine oxidase inhibitory properties of this versatile scaffold, a series of furanochalcones were synthesized. The results demonstrate that these furan substituted phenylpropenones exhibited moderate to good inhibitory activities towards MAO-B, but showed weak or no inhibition of the MAO-A enzyme. The most active compound, 2E-3-(5-chlorofuran-2-yl)-1-(3-chlorophenyl)prop-2-en-1-one, exhibited an IC50 value of 0.174 lM for the inhibition of MAO-B and 28.6 lM for the inhibition of MAO-A. Interestingly, contrary to data previously reported for chalcones, these furan substituted derivatives acted as reversible inhibitors, while kinetic analysis revealed a competitive mode of binding
    URI
    http://hdl.handle.net/10394/13691
    https://www.sciencedirect.com/science/article/pii/S0960894X13007713
    https://doi.org/10.1016/j.bmcl.2013.06.050
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