Synthesis and evaluation of antimicrobial properties of some azole derivatives

  • Mohd Imran
  • Abdulhakim Bawadekji
  • Nawaf Alotaibi
Keywords: Synthesis, Imidazole, Thiazole, Triazole, Antimicrobials


Purpose: To synthesize new azole derivatives and determine their antimicrobial properties.

Methods: The reaction of the intermediates (2a-2c) with 3a-3c in acetone/potassium carbonate solution yielded 4a-4i, which were characterized using Fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR)) and mass spectrometry (MS). Compounds 4a-4i were assessed for their antibacterial and antifungal effects using the sequential dilution technique, relative to ofloxacin and ketoconazole.

Results: The spectral data for 4a-4i were consistent with the assigned structures. The MIC of compound 4h (10 μg/ml) was similar to that of ketoconazole against Aspergillus flavus, Penicillium citrinum, and Aspergillus niger. The MIC value of compound 4b (10 μg/ml) for Penicillium citrinum was comparable to that of ketoconazole while the MIC value of compound 4d against Staphylococcus aureus and Escherichia coli (20 μg/ml) was equivalent to the corresponding MIC value for ofloxacin.

Conclusion: The synthesized compounds bearing boronic acid moiety are good antimicrobial agents. Accordingly, further investigation into the thiazole-imidazole or thiazole-triazole derivatives bearing boronic acid moiety is suggested.

Keywords: Synthesis, Imidazole, Thiazole, Triazole, Antimicrobials


Journal Identifiers

eISSN: 1596-9827
print ISSN: 1596-5996