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

J Med Chem. 2002 Mar 14;45(6):1180-3. doi: 10.1021/jm015578d.

Abstract

3-(1H-Pyrrol-1-yl)-2-oxazolidinones 1aminus signi 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 1aminus signi 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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Humans
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / chemical synthesis*
  • Monoamine Oxidase Inhibitors / pharmacology
  • Oxazolidinones / chemical synthesis*
  • Oxazolidinones / pharmacology
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology

Substances

  • Monoamine Oxidase Inhibitors
  • Oxazolidinones
  • Pyrroles
  • Monoamine Oxidase