Scholarlink

<p>A novel group of <i>N</i>-4-piperazinyl norfloxacin analogues bearing <i>N</i>-4-piperazinyl-(3-arylidene/alkylidene acrylonitrile) moieties was synthesized. Antibacterial screening revealed that four compounds were more effective against <i>S. aureus</i> with minimum inhibitory concentration (MIC) values of 0.33–0.81 µM than the parent norfloxacin with MIC value of 0.98 µM. Also, three compounds showed superior efficacy against the Gram-negative <i>E. coli</i> with MIC values of 1.28–1.62 µM, surpassing norfloxacin with MIC value of 1.96&#xa0;µM. Furthermore, two compounds exhibited more potency against <i>K. pneumoniae</i> with MICs of 1.35 and 1.62 µM, respectively, compared to norfloxacin with MIC = 3.92 µM. Moreover, six compounds showed better activity against <i>P. aeruginosa</i>, with MIC values of 2.42–3.42 µM, compared to norfloxacin (MIC = 3.92&#xa0;µM). In addition, four compounds exhibited superior minimum bactericidal activity (MBA) against the tested bacterial strains when compared to norfloxacin. Docking studies showed good affinity of the tested compounds to the <i>S. aureus</i> gyrase enzyme active binding site (PDB ID: 2XCT), which goes ahead with the data of the mechanistic study for the most potent compounds which revealed the effectiveness of one compound to poison DNA gyrase and topoisomerase IV, slightly better than norfloxacin.</p> Graphical abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

New norfloxacin analogues based on N-4-piperazinyl-(3-arylidene/alkylidene acrylonitrile) moieties: design, synthesis, antibacterial evaluation, and in silico studies

  • 期刊论文

  • 发表日期：

    2025年5月7日

查看全文
  • Ahmed M. El-Saghier,
  • Laila Abosella,
  • Amany M. Hamed,
  • Esmail O. Elakesh,
  • Gamal El-Din A. Abuo-Rahma,
  • Magda H. Abdellattif,
  • Hossameldin A. Aziz

摘要

A novel group of N-4-piperazinyl norfloxacin analogues bearing N-4-piperazinyl-(3-arylidene/alkylidene acrylonitrile) moieties was synthesized. Antibacterial screening revealed that four compounds were more effective against S. aureus with minimum inhibitory concentration (MIC) values of 0.33–0.81 µM than the parent norfloxacin with MIC value of 0.98 µM. Also, three compounds showed superior efficacy against the Gram-negative E. coli with MIC values of 1.28–1.62 µM, surpassing norfloxacin with MIC value of 1.96 µM. Furthermore, two compounds exhibited more potency against K. pneumoniae with MICs of 1.35 and 1.62 µM, respectively, compared to norfloxacin with MIC = 3.92 µM. Moreover, six compounds showed better activity against P. aeruginosa, with MIC values of 2.42–3.42 µM, compared to norfloxacin (MIC = 3.92 µM). In addition, four compounds exhibited superior minimum bactericidal activity (MBA) against the tested bacterial strains when compared to norfloxacin. Docking studies showed good affinity of the tested compounds to the S. aureus gyrase enzyme active binding site (PDB ID: 2XCT), which goes ahead with the data of the mechanistic study for the most potent compounds which revealed the effectiveness of one compound to poison DNA gyrase and topoisomerase IV, slightly better than norfloxacin.

Graphical abstract