3-(1H-Pyrrol-1-yl)-2-oxazolidinones 1a−i have been synthesized as pyrrole analogues of toloxatone (Humoryl), an antidepressant agent belonging to the 3-phenyl-2-oxazolidinone class, and their monoamine oxidase (MAO) type A and B inhibitory activities have been evaluated. The majority of 1a−i showed inhibitory activity against the A isoform of the enzyme higher than that exerted against the MAO-B, the sole exception being the (S)-5-aminomethylderivative 1d. (R)-5-Methoxymethyl-3-(1H-pyrrol-1-yl)-2-oxazolidinone 1b, the most potent among test derivatives, was 78-fold more potent than toloxatone.
3-(1H-Pyrrol-1-yl)-2-oxazolidinones as Reversible, Highly Potent, and Selective Inhibitors of Monoamine Oxidase Type A
SBARDELLA, Gianluca;
2002-01-01
Abstract
3-(1H-Pyrrol-1-yl)-2-oxazolidinones 1a−i have been synthesized as pyrrole analogues of toloxatone (Humoryl), an antidepressant agent belonging to the 3-phenyl-2-oxazolidinone class, and their monoamine oxidase (MAO) type A and B inhibitory activities have been evaluated. The majority of 1a−i showed inhibitory activity against the A isoform of the enzyme higher than that exerted against the MAO-B, the sole exception being the (S)-5-aminomethylderivative 1d. (R)-5-Methoxymethyl-3-(1H-pyrrol-1-yl)-2-oxazolidinone 1b, the most potent among test derivatives, was 78-fold more potent than toloxatone.File in questo prodotto:
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