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Quinoline-2-one derivatives as promising antibacterial agents against multidrug-resistant Gram-positive bacterial strains

  • Clinical Microbiology - Research Paper
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Abstract

This study describes the discovery of a variety of quinoline2-one derivatives with significant antibacterial action vs a spectrum of multidrug-resistant Gram-positive bacterial strains, especially methicillin-resistant Staphylococcus aureus (MRSA). Compounds 6c, 6l, and 6o exhibited significant antibacterial activity versus the Gram-positive bacterial pathogens evaluated. In comparison to the reference daptomycin, compound 6c demonstrated the most effective activity among the assessed derivatives, with MIC concentrations of 0.75 μg/mL versus MRSA and VRE and 2.50 μg/mL against MRSE. We also reported on these compounds’ biofilm and dihydrofolate reductase inhibitory activities. Compound 6c showed the greatest antibiofilm action in a dose-dependent way and a substantial decrease of biofilm development in the MRSA ACL51 strain at concentrations of 0.5, 0.25, and 0.12 MIC, with reductions of 79%, 55%, and 38%, consecutively, whereas the corresponding values for vancomycin were 20%, 12%, and 9%. These findings imply that these quinoline compounds could be used to develop a new category of antibiotic representatives to prevent Gram-positive drug-resistant bacterial strains.

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Acknowledgements

Professor Dr. Bahaa G. M. Youssif, and Dr. Elbastawesy M.A., Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut, Egypt, are gratefully acknowledged for providing compounds 6c, 6i, 6l, and 6o for biological assays.

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  1. Medical Laboratory Technology Department, Applied Medical Science College, Northern Border University, Arar, Saudi Arabia

    Hayat Ali Alzahrani

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Alzahrani, H.A. Quinoline-2-one derivatives as promising antibacterial agents against multidrug-resistant Gram-positive bacterial strains. Braz J Microbiol 54, 2799–2805 (2023). https://doi.org/10.1007/s42770-023-01132-w

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