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<p>Herein, 8-[(1H-benzo[d]imidazol-2-yl)methoxy] quinoline derivatives as a future antimicrobial agents has been reported. All the freshly synthesized samples were appropriately characterized with assistance of IR, NMR, mass and CHN analysis techniques. The prediction of antimicrobial activity of the prepared compounds has been assessed by using in silico molecular docking studies against 3U2K protein, which revealed significant interactions of the compounds, especially compound <b>5i</b>, at the active site pocket of the protein showing with a reasonable conformity similar to the co-crystal ligand interactions. Further, all the prepared samples were screened for in vitro antimicrobial applications with various bacterial and fungal strains. Among all the newly synthesized series <b>5a-j</b>, compound <b>5i</b> with two bromo groups at 5th and 7th position of quinoline moiety emerged as the best compound among the tested strains. The SAR studies indicate that placing electron-withdrawing bulky groups at the appropriate positions, along with combining two heterocyclic moieties, enhances the bioactivity of the synthesized compounds.</p>

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Design, synthesis and characterization of 8-[(1H-benzo[d]imidazol-2-yl)methoxy] quinoline derivatives as antimicrobial agents

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年2月19日

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  • T. Prashanth,
  • V. Lakshmi Ranganatha,
  • Mohammed Al-Ghorbani,
  • S. Girish,
  • Hussien Ahmed Khamees,
  • Shaukath Ara Khanum

摘要

Herein, 8-[(1H-benzo[d]imidazol-2-yl)methoxy] quinoline derivatives as a future antimicrobial agents has been reported. All the freshly synthesized samples were appropriately characterized with assistance of IR, NMR, mass and CHN analysis techniques. The prediction of antimicrobial activity of the prepared compounds has been assessed by using in silico molecular docking studies against 3U2K protein, which revealed significant interactions of the compounds, especially compound 5i, at the active site pocket of the protein showing with a reasonable conformity similar to the co-crystal ligand interactions. Further, all the prepared samples were screened for in vitro antimicrobial applications with various bacterial and fungal strains. Among all the newly synthesized series 5a-j, compound 5i with two bromo groups at 5th and 7th position of quinoline moiety emerged as the best compound among the tested strains. The SAR studies indicate that placing electron-withdrawing bulky groups at the appropriate positions, along with combining two heterocyclic moieties, enhances the bioactivity of the synthesized compounds.