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<p>The structure–activity (antinociceptive) relationship of a series of structural isomers of NMDA-receptor ligands was studied in thermal and mechanical somatic pain models in mice. It was shown that the chemical structure of imidazole-4,5-dicarboxylic acid derivatives had a significant effect on the manifestation of antinociceptive activity by the compounds. The activity changed by two orders of magnitude in a series of isomeric compounds that differed not in the pharmacophore groups but only in the alkyl substituents in the 1- and 2-positions. It was shown that compounds containing linear propyl radicals in the 1- and 2-positions of the imidazole ring had the greatest antinociceptive potential. Compounds containing branched and cyclic propyl radicals had the lowest activity. The analgesic effects of structural isomers of <i>bis</i>-methylamide 1-propylimidazole-4,5-dicarboxylic acid were comparable or superior to those of the reference drugs analgin and ketorolac.</p>

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Search for New Analgesics Among Imidazole-4,5-Dicarboxylic Acid Derivatives

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • M. A. Brusina,
  • L. G. Kubarskaya,
  • A. M. Potapkin,
  • L. B. Piotrovskiy,
  • E. V. Litasova

摘要

The structure–activity (antinociceptive) relationship of a series of structural isomers of NMDA-receptor ligands was studied in thermal and mechanical somatic pain models in mice. It was shown that the chemical structure of imidazole-4,5-dicarboxylic acid derivatives had a significant effect on the manifestation of antinociceptive activity by the compounds. The activity changed by two orders of magnitude in a series of isomeric compounds that differed not in the pharmacophore groups but only in the alkyl substituents in the 1- and 2-positions. It was shown that compounds containing linear propyl radicals in the 1- and 2-positions of the imidazole ring had the greatest antinociceptive potential. Compounds containing branched and cyclic propyl radicals had the lowest activity. The analgesic effects of structural isomers of bis-methylamide 1-propylimidazole-4,5-dicarboxylic acid were comparable or superior to those of the reference drugs analgin and ketorolac.