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<p>A series of 17 aryl aziridines bearing electron-withdrawing groups at the C1 position, including five novel compounds, were synthesized in moderate to excellent yields through thermal cycloaddition reactions of aryl azides and alkenes. All synthesized compounds were characterized using spectroscopic methods. The antimicrobial properties of the compounds were evaluated against three bacterial strains (<i>Escherichia coli</i>, <i>Staphylococcus aureus</i>, and <i>Kocuria rhizophila</i>), as well as one fungal strain (<i>Candida albicans</i>). The zone of inhibition, minimum inhibitory concentration, and minimum bactericidal concentration values of aryl aziridines were determined. Among the tested compounds, aziridine-2-COOMe derivatives demonstrated the most pro-nounced antimicrobial efficacy against <i>E. coli</i> and <i>C. albicans</i>, whereas aziridine-2-CONMe<sub>2</sub> derivatives were the most potent compounds against <i>S. aureus</i> and <i>K. rhizophila</i>. A brief study of the structure–activity rela-tionship between the tested aziridines and antimicrobial activity is provided.</p>

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Design, Synthesis, and Antimicrobial Evaluation of Aryl Aziridines Bearing Electron-Withdrawing C-Substituents

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • Lalita Radtanajiravong,
  • Krissana Khoothiam,
  • Chutamas Thepmalee,
  • Jeerasak Pratummart,
  • Supissara Phongpaew

摘要

A series of 17 aryl aziridines bearing electron-withdrawing groups at the C1 position, including five novel compounds, were synthesized in moderate to excellent yields through thermal cycloaddition reactions of aryl azides and alkenes. All synthesized compounds were characterized using spectroscopic methods. The antimicrobial properties of the compounds were evaluated against three bacterial strains (Escherichia coli, Staphylococcus aureus, and Kocuria rhizophila), as well as one fungal strain (Candida albicans). The zone of inhibition, minimum inhibitory concentration, and minimum bactericidal concentration values of aryl aziridines were determined. Among the tested compounds, aziridine-2-COOMe derivatives demonstrated the most pro-nounced antimicrobial efficacy against E. coli and C. albicans, whereas aziridine-2-CONMe2 derivatives were the most potent compounds against S. aureus and K. rhizophila. A brief study of the structure–activity rela-tionship between the tested aziridines and antimicrobial activity is provided.