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Synthesis and Monoamine Oxidase Inhibition Properties of (Sulfamoylphenyl)quinoline-4-carboxylic Acids

  • J. Efimova,
  • A. Shetnev,
  • M. Korsakov,
  • E. Petersen,
  • A. Petzer,
  • J. P. Petzer

摘要

Abstract

By reaction between acetylbenzenesulfonamides with several substituted isatins, we have synthesized a series of 22 primary sulfonamides, 16 of which were tested for inhibition activity against MAO-A and MAO-B. At the same time, in order to diversify the resulting structures, we have carried out decarboxylation as well as further functionalization at the carboxylic acid. The results of the study show that methyl 6-chloro-2-(3-sulfamoylphenyl)quinoline-4-carboxylate selectively inhibited MAO-B with a value of IC50 = 13.7 μM.