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Abstract <p><b>Objective:</b> To address the serious challenge of antibiotic resistance, this study aimed to synthesize a series of novel naphthoquinone-4-aminosulfonamide derivatives and evaluate their anti-<i>Helicobacter pylori</i> (<i>H. pylori</i>) activity. <b>Methods:</b> The target derivatives were synthesized using benzenesulfonyl chlorides, <i>N</i>-Boc-1,4-butanediamine, and 2-chloro-1,4-naphthoquinone as starting materials. All synthesized compounds were characterized by HRMS and NMR spectroscopy. Antibacterial activity was assessed using the broth microdilution method. <b>Results and Discussion:</b> Nine target compounds were successfully synthesized. All compounds exhibited significant inhibitory activity against <i>H. pylori</i>, with minimum inhibitory concentration (MIC) values ranging from 4 to 16 μg/mL. <b>Conclusions:</b> These results indicate the potential of the synthesized derivatives as promising candidates for novel anti-<i>H. pylori</i> therapies.</p>

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Synthesis and Biological Evaluation of Novel Naphthoquinone-4-aminosulfonamide Derivatives as Antibacterial Agents

  • 期刊论文

  • 发表日期：

    2026年1月22日

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  • Jiazi Luo,
  • Meishan Li,
  • Yi Wei,
  • Yuban Lei,
  • Haiying Luo,
  • Kelin Lu,
  • Zheng Liu,
  • Gang Wei

摘要

Abstract

Objective: To address the serious challenge of antibiotic resistance, this study aimed to synthesize a series of novel naphthoquinone-4-aminosulfonamide derivatives and evaluate their anti-Helicobacter pylori (H. pylori) activity. Methods: The target derivatives were synthesized using benzenesulfonyl chlorides, N-Boc-1,4-butanediamine, and 2-chloro-1,4-naphthoquinone as starting materials. All synthesized compounds were characterized by HRMS and NMR spectroscopy. Antibacterial activity was assessed using the broth microdilution method. Results and Discussion: Nine target compounds were successfully synthesized. All compounds exhibited significant inhibitory activity against H. pylori, with minimum inhibitory concentration (MIC) values ranging from 4 to 16 μg/mL. Conclusions: These results indicate the potential of the synthesized derivatives as promising candidates for novel anti-H. pylori therapies.