Abstract
Novel 1-trifluoromethyl-4-quinolone derivatives (8a,b) were synthesized, and the antibacterial activity of each was evaluated. An oxidative desulfurization-fluorination reaction was employed to introduce a trifluoromethyl group at the N-1 position as a key step. Among the derivatives, 8a was found to exhibit antibacterial activity comparable to that of norfloxacin (1) against Staphylococcus aureus Smith, Streptococcus pneumoniae IID1210, and Escherichia coli NIHJ JC-2.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Carboxylic Acids / chemical synthesis*
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Carboxylic Acids / chemistry
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Carboxylic Acids / pharmacology
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Escherichia coli / drug effects
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Microbial Sensitivity Tests
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Pseudomonas aeruginosa / drug effects
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Quinolones / chemical synthesis*
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Quinolones / chemistry
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Quinolones / pharmacology
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Staphylococcus aureus / drug effects
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Streptococcus pneumoniae / drug effects
Substances
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Anti-Bacterial Agents
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Carboxylic Acids
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Quinolones