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2000
Volume 31, Issue 32
  • ISSN: 1381-6128
  • E-ISSN: 1873-4286

Abstract

Introduction

The increasing use of antibiotics coupled with the lack of innovative and effective antimicrobial agents has increased the development of antimicrobial resistance (AMR) worldwide. To overcome the AMR-associated prolonged disease duration and increased mortality rates, new antimicrobial agents are in high demand. In this context, hydrazone and oxadiazole derivatives are endowed with remarkable biocidal activity, becoming profitable scaffolds in the design of antimicrobial candidates.

Methods

In this study, the antimicrobial effects of N-acyl hydrazones - and 2,5-disubstituted 1,3,4-oxadiazoles - against ATCC 25922, ATCC 29213, ATCC 6633, and clinically isolated , , and were evaluated. For this purpose, Kirby-Bauer disc diffusion and MIC tests were carried out, indicating that most of these compounds were active against tested microorganisms. Particularly, several compounds proved active against , whereas showed higher resistance. The genotoxic potential of most active compounds was determined by alkaline comet assay, and they were found to be non-toxic at studied concentrations.

Results

Finally, molecular docking and dynamics (MD) studies identified four compounds as potential inhibitors of bacterial DNA gyrase B (GyrB).

Conclusion

Further exploration of molecular determinants revealed favourable drug-like properties, highlighting the potential of these molecules for subsequent hit-to-lead optimization studies.

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Biological Evaluation and Computational Modelling Studies on N-acyl Hydrazone and 2,5-Disubstituted 1,3,4-Oxadiazole Derivatives as Non-toxic Antimicrobial Agents
Curr. Pharm. Des. 31, 2611 (2025); https://doi.org/10.2174/0113816128361524250131110036
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  • Article Type:     Research Article
Keyword(s): antimicrobial activity; antimicrobial resistance; bacterial DNA gyrase; ESKAPE; Hydrazones; tetracyclines

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