Abstract <p>A series of substituted (<i>Z</i>)-1-benzyl-3-{[3-(4-nitrophenyl)-1-phenyl-1<i>H</i>-pyrazol-4-yl]methylidene}­pyrrolidine-2,5-dione derivatives <b>8a–8j</b> were synthesized and characterized. Their in vitro antimicrobial activity was evaluated against Gram-positive bacteria (<i>Staphylococcus aureus</i>, <i>Streptococcus pyogenes</i>), Gram-negative bacteria (<i>Escherichia coli</i>, <i>Pseudomonas aeruginosa</i>), and fungal species (<i>Candida albicans</i>, <i>Aspergillus clavatus</i>, <i>Aspergillus niger</i>). Compounds <b>8d</b> and <b>8i</b> exhibited significant antibacterial activity compared with the other derivatives. The antimicrobial activity was assessed by measuring zones of inhibition and compared with standard drugs. Furthermore, in silico molecular docking studies were performed to analyze the binding interactions of the synthesized compounds with selected bacterial (PDB IDs: 1JIJ, 4ROT, 1KZN, 4JVI) and fungal (PDB IDs: 5C5G, 1IYL, 1UKC) target proteins in order to elucidate their potential mechanism of action.</p>

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Synthesis, Characterization, and Biological Evaluation of Substituted (Z)-1-Benzyl-3-{[3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl]methylidene}pyrrolidine-2,5-diones

  • H. A. Modi,
  • D. V. Pathak,
  • P. D. Suradiya,
  • D. B. Chhag,
  • A. K. Mahida,
  • G. L. Jadav

摘要

Abstract

A series of substituted (Z)-1-benzyl-3-{[3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl]methylidene}­pyrrolidine-2,5-dione derivatives 8a–8j were synthesized and characterized. Their in vitro antimicrobial activity was evaluated against Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and fungal species (Candida albicans, Aspergillus clavatus, Aspergillus niger). Compounds 8d and 8i exhibited significant antibacterial activity compared with the other derivatives. The antimicrobial activity was assessed by measuring zones of inhibition and compared with standard drugs. Furthermore, in silico molecular docking studies were performed to analyze the binding interactions of the synthesized compounds with selected bacterial (PDB IDs: 1JIJ, 4ROT, 1KZN, 4JVI) and fungal (PDB IDs: 5C5G, 1IYL, 1UKC) target proteins in order to elucidate their potential mechanism of action.