3-Coumaranone derivatives as inhibitors of monoamine oxidase

作者: Lesetja Legoabe , Adriaan Van Dyk , Anél Petzer , Jacobus Petzer

DOI: 10.2147/DDDT.S89961

关键词:

摘要: The present study examines the monoamine oxidase (MAO) inhibitory properties of a series 20 3-coumaranone [benzofuran-3(2H)-one] derivatives. derivatives are structurally related to α-tetralone and 1-indanone derivatives, which have recently been shown potently inhibit MAO, with selectivity for MAO-B (in preference MAO-A isoform). 3-Coumaranones similarly found selectively human half-maximal concentration (IC50) values 0.004-1.05 µM. Nine compounds exhibited IC50 100 µM, only one compound possessing an IC50<1 For selected it is established that inhibition reversible since dialysis enzyme-inhibitor mixtures almost completely restores enzyme activity. On basis profiles potent action, may be concluded suitable leads development selective inhibitors as potential treatment disorders such Parkinson's disease Alzheimer's disease.

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