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<p>In this study, coumarin derivatives containing amide and sulfanilamide moieties were designed and synthesized, and their antibacterial activities were systematically evaluated. Among the synthesised compounds, compound <b>A7</b> exhibited good inhibitory activity against <i>Psa</i>, with an EC<sub>50</sub> value of 59.4&#xa0;mg/L. Compound <b>A2</b> presented the most potent antibacterial effect against <i>Xoc</i>, with an EC<sub>50</sub> value of 43.2&#xa0;mg/L. Compound <b>A3</b> showed notable efficacy against <i>Xac</i>, with an EC<sub>50</sub> value of 53.2&#xa0;mg/L. Further mechanistic studies involving scanning electron microscopy (SEM) and extracellular conductivity (EC) measurements revealed that <b>A2</b> induced morphological deformation and alterations in membrane permeability alterations in <i>Xoc</i> cells, suggesting a potential disruption of bacterial membrane integrity. Additionally, the structure–activity relationship (SAR) of these derivatives was elucidated using 3D-QSAR model, providing insights for further structural optimization. Furthermore, the chemical reactivity of potential bioactive compounds was evaluated using density functional theory (DFT).</p> Graphical Abstract <p></p>

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Design, synthesis and anti-plant-bacterial (Xoc, Xac, Psa) activity of coumarins derivatives containing amide and sulfonamide moieties

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月2日

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  • Song Bai,
  • Miaohe Zhang,
  • Rong Wu,
  • Suran Wan,
  • Lijun Chen,
  • Shouying Tang,
  • Xian Wei,
  • Shuang Feng,
  • Miao Li

摘要

In this study, coumarin derivatives containing amide and sulfanilamide moieties were designed and synthesized, and their antibacterial activities were systematically evaluated. Among the synthesised compounds, compound A7 exhibited good inhibitory activity against Psa, with an EC50 value of 59.4 mg/L. Compound A2 presented the most potent antibacterial effect against Xoc, with an EC50 value of 43.2 mg/L. Compound A3 showed notable efficacy against Xac, with an EC50 value of 53.2 mg/L. Further mechanistic studies involving scanning electron microscopy (SEM) and extracellular conductivity (EC) measurements revealed that A2 induced morphological deformation and alterations in membrane permeability alterations in Xoc cells, suggesting a potential disruption of bacterial membrane integrity. Additionally, the structure–activity relationship (SAR) of these derivatives was elucidated using 3D-QSAR model, providing insights for further structural optimization. Furthermore, the chemical reactivity of potential bioactive compounds was evaluated using density functional theory (DFT).

Graphical Abstract