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<p>This research highlights the significance of 1,5-benzodiazepines and their remarkable antimicrobial potential. In this study, we meticulously designed 13 unique 1,5-benzodiazepine derivatives and subjected them to comprehensive molecular-docking studies. Four of these derivatives exhibit the most promising activity in in silico antibacterial and antifungal assessments. The designed compounds were synthesized by a strategic combination of various substituted ñhalcones with <i>o</i>-phenylenediamines to construct novel 1,5-benzodiazepines. The synthesized compounds underwent rigorous characterization using IR, NMR, and mass spectra. To assess their efficacy, the compounds were subjected to in vitro antibacterial evaluations against Gram-positive bacteria (<i>S. aureus</i> and <i>B. subtilis</i>) and Gram-negative bacteria (<i>E. coli</i> and <i>S. typhi</i>). Additionally, in vitro antifungal activities against <i>A. niger</i>, <i>A. flavus</i>, <i>P. chrysogenum</i>, and <i>F. moniliform</i> were evaluated, with ciprofloxacin and fluconazole serving as reference standards. Among these compounds, <b>4a</b> exhibited exceptional antibacterial activity with a minimum inhibitory concentration (MIC) of 6.25 μg/mL, whereas <b>4c</b> displayed noteworthy antifungal activity at the same MIC. These findings showed that 1,5-benzodiazepine derivatives are promising candidates for novel antimicrobial agents, offering new avenues in the battle against infectious diseases and antimicrobial resistance.</p>

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Investigating the Bioactivity of 1,5-Benzodiazepine Derivatives: Synthesis, Characterization, Molecular Docking, and Antimicrobial Evaluation

  • 期刊论文

  • 发表日期：

    2025年11月1日

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  • Bharath Kumar Chagaleti,
  • Aswani Ankireddy,
  • Samyuktha,
  • Sri Mounika Bellapukonda,
  • N. Raghavendra Babu,
  • K. Varalakshmi Devi

摘要

This research highlights the significance of 1,5-benzodiazepines and their remarkable antimicrobial potential. In this study, we meticulously designed 13 unique 1,5-benzodiazepine derivatives and subjected them to comprehensive molecular-docking studies. Four of these derivatives exhibit the most promising activity in in silico antibacterial and antifungal assessments. The designed compounds were synthesized by a strategic combination of various substituted ñhalcones with o-phenylenediamines to construct novel 1,5-benzodiazepines. The synthesized compounds underwent rigorous characterization using IR, NMR, and mass spectra. To assess their efficacy, the compounds were subjected to in vitro antibacterial evaluations against Gram-positive bacteria (S. aureus and B. subtilis) and Gram-negative bacteria (E. coli and S. typhi). Additionally, in vitro antifungal activities against A. niger, A. flavus, P. chrysogenum, and F. moniliform were evaluated, with ciprofloxacin and fluconazole serving as reference standards. Among these compounds, 4a exhibited exceptional antibacterial activity with a minimum inhibitory concentration (MIC) of 6.25 μg/mL, whereas 4c displayed noteworthy antifungal activity at the same MIC. These findings showed that 1,5-benzodiazepine derivatives are promising candidates for novel antimicrobial agents, offering new avenues in the battle against infectious diseases and antimicrobial resistance.