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<p>The urgent global health threat of antimicrobial resistance demands innovative therapeutic strategies. Herein, we report the design, synthesis, and biological evaluation (antibacterial and antifungal activities) of two series of alkynyl-linked aminoguanidine derivatives. A critical structure–activity relationship (SAR) was revealed: the exposure of the aminoguanidine group is paramount for activity. In vitro antibacterial and antifungal activities revealed that the imidazol-2-hydrazine series exhibited inhibition against both Gram-positive and Gram-negative bacteria, with minimum inhibitory concentration (MIC) ranging from 2 to 64&#xa0;μg/mL. Among them, compound <b>IIh</b> exhibited a MIC of 2&#xa0;μg/mL against both <i>S. aureus</i> CMCC 25923 and <i>Enterococcus faecalis</i> CMCC 29212, and also demonstrated significant antifungal activity against <i>Candida albicans</i> SC5314 with a MIC of 2&#xa0;μg/mL. Time-kill kinetics established the rapid bactericidal nature of <b>IIh</b>, achieving complete eradication of <i>E. coli</i> and <i>S. aureus</i> within 1–2&#xa0;h. Furthermore, <b>IIh</b> significantly inhibited biofilm formation and compromised bacterial membrane integrity, leading to the leakage of cytoplasmic proteins and nucleic acids. Checkerboard assays revealed a synergistic relationship between <b>IIh</b> and conventional antibiotics, reducing their effective MICs. As a promising candidate for combating resistant infections, <b>IIh</b> deserves further efficacy and safety studies.</p>

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Novel aminoguanidine derivatives containing alkynyl moiety: synthesis and evaluation of antibacterial and antifungal activities

  • 期刊论文

  • 发表日期：

    2026年2月4日

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  • Hongling Lai,
  • Jie Zheng,
  • Yi Li,
  • Dandan Chen,
  • Yajing Tian,
  • Yuanying Jiang,
  • Xianqing Deng,
  • Mingxia Song,
  • Xunli Xiao

摘要

The urgent global health threat of antimicrobial resistance demands innovative therapeutic strategies. Herein, we report the design, synthesis, and biological evaluation (antibacterial and antifungal activities) of two series of alkynyl-linked aminoguanidine derivatives. A critical structure–activity relationship (SAR) was revealed: the exposure of the aminoguanidine group is paramount for activity. In vitro antibacterial and antifungal activities revealed that the imidazol-2-hydrazine series exhibited inhibition against both Gram-positive and Gram-negative bacteria, with minimum inhibitory concentration (MIC) ranging from 2 to 64 μg/mL. Among them, compound IIh exhibited a MIC of 2 μg/mL against both S. aureus CMCC 25923 and Enterococcus faecalis CMCC 29212, and also demonstrated significant antifungal activity against Candida albicans SC5314 with a MIC of 2 μg/mL. Time-kill kinetics established the rapid bactericidal nature of IIh, achieving complete eradication of E. coli and S. aureus within 1–2 h. Furthermore, IIh significantly inhibited biofilm formation and compromised bacterial membrane integrity, leading to the leakage of cytoplasmic proteins and nucleic acids. Checkerboard assays revealed a synergistic relationship between IIh and conventional antibiotics, reducing their effective MICs. As a promising candidate for combating resistant infections, IIh deserves further efficacy and safety studies.