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<p>The search for treatments for anxiety-depressive disorders and dementia-related disorders is a pressing issue in modern pharmacology. Astudy using laboratory rats examined the psychotropic properties of 4-substituted pyroglutamic acids and their amides and peptides and identified a link between chemical structure and psychotropic activity. Among the 4-amino-1-arylpyroglutamic acids, the 4-fluorophenyl, 3-fluorophenyl, 4-bromophenyl, and 3-bromophenyl derivatives demonstrated the greatest anxiolytic activity in the elevated plus maze and Vogel tests, while the 3-hydroxyphenyl and 4-fluorophenyl derivatives exhibited the most pronounced nootropic effects. Among the amides and peptides, (2<i>S</i>,4<i>S</i>)-4-amino-1-(4-fluorophenyl)pyroglutamyl-(<i>S</i>)-histidine was identified as having the highest anxiolytic activity, as was (2<i>S</i>,4<i>S</i>)-4-[(methyl)-(phenyl)amino]pyroglutamylmorpholine, which exhibited the greatest nootropic activity. The results indicated that the studied pyroglutamic acid derivatives hold promise as potential agents for the treatment of anxiety and cognitive disorders.</p>

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Psychotropic Activity of 4-Substituted Pyroglutamic Acids and Their Amides and Peptides

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • V. P. Krasnov,
  • A. Yu. Vigorov,
  • I. A. Nizova,
  • D. A. Bakulin,
  • D. D. Samarkin,
  • I. N. Tyurenkov

摘要

The search for treatments for anxiety-depressive disorders and dementia-related disorders is a pressing issue in modern pharmacology. Astudy using laboratory rats examined the psychotropic properties of 4-substituted pyroglutamic acids and their amides and peptides and identified a link between chemical structure and psychotropic activity. Among the 4-amino-1-arylpyroglutamic acids, the 4-fluorophenyl, 3-fluorophenyl, 4-bromophenyl, and 3-bromophenyl derivatives demonstrated the greatest anxiolytic activity in the elevated plus maze and Vogel tests, while the 3-hydroxyphenyl and 4-fluorophenyl derivatives exhibited the most pronounced nootropic effects. Among the amides and peptides, (2S,4S)-4-amino-1-(4-fluorophenyl)pyroglutamyl-(S)-histidine was identified as having the highest anxiolytic activity, as was (2S,4S)-4-[(methyl)-(phenyl)amino]pyroglutamylmorpholine, which exhibited the greatest nootropic activity. The results indicated that the studied pyroglutamic acid derivatives hold promise as potential agents for the treatment of anxiety and cognitive disorders.