3-(1H-pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A

被引：49

作者：

Mai, A

Artico, M

Esposito, M

Sbardella, G

Massa, S

Befani, O

Turini, P

Giovannini, V

Mondovì, B

机构：

[1] Univ Roma La Sapienza, Dipartimento Studi Farmaceut, I-00185 Rome, Italy

[2] Univ Salerno, Dipartimento Sci Farmaceut, I-84084 Fisciano, SA, Italy

[3] Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy

[4] Univ Roma La Sapienza, CNR, Dipartimento Sci Biochim A Rossi Fanelli, I-00185 Rome, Italy

[5] Univ Roma La Sapienza, CNR, Ctr Mol Biol, I-00185 Rome, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 06期

关键词：

D O I：

10.1021/jm015578d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 la-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-(1-H-pyrrol-1-yl)-2-oxazolidinone 1b, the most potent among test derivatives, was 78-fold more potent than toloxatone.

引用

页码：1180 / 1183

页数：4

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