Synthesis and characterization of some hydroxypyridone derivatives and their evaluation as antimicrobial agents

Abstract

The synthesis, in vitro antimicrobial activities of some novel hydroxy pyridines supported with various pharmacophores is described. Twenty-six out of the tested 58 compounds exhibited variable inhibitory effects on the growth of the tested Gram positive and Gram negative bacteria. The tested compounds revealed better activity against the Gram positive rather than the Gram negative strains. The synthesized hydroxypyridones have shown very significant inhibitory effect against Staphylococcus aureus and Bacillus subtilis. Twelve compounds namely; 5d, 5f, 6a, 6b, 8b, 18b, 18c, 19c, 21d, 22b, 22d and 23d were able to produce appreciable growth inhibitory activity against Candida albicans when compared to Clotrimazole. Among these, 22d proved to be the most potent antifungal agent.

Keywords::

• Synthesis
• hydroxypyridones
• antibacterial
• antifungal

Acknowledgements

The authors are very grateful to the authorities of the Institute of Research and Consultation, King Abdulaziz University, Jeddah, Saudi Arabia, as well as SABIC group of companies, for the financial support of this research. Extendable thanks are due to the staff members of the Department of Health and Human Services, National Cancer Institute (NCI), Bethesda, Maryland, U.S.A. for carrying out the anticancer screening of the newly synthesized compounds.

Declaration of interest

The authors report no conflicts of interest.