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Synthesis and Analgesic Activity of 4-(3-Acyl-2-Aryl-4-Hydroxy-5-Oxo-2,5-Dihydro-1H-Pyrrol-1-yl)Benzoic Acids

  • V. L. Gein,
  • D. V. Chalkov,
  • A. V. Romanova,
  • O. V. Bobrovskaya,
  • S. V. Chaschina

摘要

4-(3-Acyl-2-aryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-1-yl)benzoic acids were synthesized by three- component reactions of acylpyruvic acid methyl esters, aromatic aldehydes, and 4-aminobenzoic acid (PABA). The structures of the compounds were determined using IR, PMR, and 13C NMR spectroscopy. Pronounced analgesic activity of the synthesized compounds was revealed. An aroyl substituent in the 3-position of the heterocycle was shown to increase the analgesic activity. All studied compounds were practically nontoxic.