Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Synthesis and evaluation of antimicrobial properties of some azole derivatives

Mohd Imran¹ , Abdulhakim Bawadekji², Nawaf Alotaibi³

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, PO Box 840, Rafha 91911; ²Department of Biological Sciences, College of Science, Northern Border University, PO Box 1321, Arar 91431; ³Department of Pharmaceutics, Faculty of Pharmacy, Northern Border University, PO Box 840, Rafha 91911, Saudi Arabia.

For correspondence:- Mohd Imran Email: imran_inderlok@yahoo.co.in Tel:+966599577945

Accepted: 25 January 2020 Published: 29 February 2020

Citation: Imran M, Bawadekji A, Alotaibi N. Synthesis and evaluation of antimicrobial properties of some azole derivatives. Trop J Pharm Res 2020; 19(2):377-382 doi: 10.4314/tjpr.v19i2.21

© 2020 The authors.
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Abstract

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