Drug Design, Development and Therapy p. 5479 - 5489 (2015)
Update date:2022-08-16
Topics:
Van Dyk, Adriaan S.
Petzer, Jacobus P.
Petzer, Anél
Legoabe, Lesetja J.
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, IC50values 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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