期刊
MEDICINAL CHEMISTRY RESEARCH
卷 25, 期 6, 页码 1274-1285出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-016-1550-x
关键词
Naphthoquinone; Antifungal; Antibacterial; Minimum inhibitory concentration; Structure-activity relationship
资金
- Consejeria de Innovacion, Ciencia y Empresa, Junta de Andalucia [P10-AGR5822]
The synthesis of 1,4-naphthoquinone derivatives is of great interest since these compounds exhibit strong activity as antimalarial, antibacterial, antifungal and anticancer agents. A series of 50 naphthoquinone derivatives was synthesized and evaluated for antibacterial and antifungal activity against Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, Staphylococcus aureus, Candida krusei, Candida parapsilosis and Cryptococcus neoformans using the broth microdilution method. The Candida species were the most susceptible microorganisms. Halogen derivatives of 1,4-naphthoquinone presented strong activity, e.g., 2-bromo-5-hydroxy-1,4-naphthoquinone, which exhibited inhibition at an MIC of 16 A mu g/mL in S. aureus, and 2-chloro-5,8-dihydroxy-1,4-naphthoquinone, with an MIC of 2 A mu g/mL in C. krusei. These compounds showed higher activity against fungi, but the antibacterial activities were very low. The study of structure-activity relationships is very important in the search for new antimicrobial drugs due to the limited therapeutic arsenal.
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