Abstract
This report describes 9H-isothiazolo[5,4-b]quinoline-3,4-diones (ITQs) containing aromatic groups at the 7-position that were prepared using palladium-catalyzed cross-coupling and tested against a panel of susceptible and resistant bacteria. In general, these compounds were more effective against Gram-positive than Gram-negative organisms. Many of the ITQs were more potent than contemporary quinolones and displayed a particularly strong antistaphylococcal activity against a clinically important, multi-drug-resistant strain. In contrast with ITQs reported previously, several of the analogues described in this Letter demonstrated low cytotoxic activity against a human cell line.
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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Anti-Bacterial Agents / toxicity
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Azo Compounds / chemical synthesis*
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Azo Compounds / chemistry
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Azo Compounds / pharmacology
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Azo Compounds / toxicity*
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Cell Line
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Escherichia coli / drug effects
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Escherichia coli / enzymology
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Humans
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Hydrocarbons, Aromatic / chemistry*
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Microbial Sensitivity Tests
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Molecular Structure
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Quinolines / chemical synthesis
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Quinolines / chemistry*
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Quinolines / pharmacology*
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Quinolines / toxicity
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Staphylococcus aureus / drug effects
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Staphylococcus aureus / enzymology
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Sulfhydryl Compounds / chemistry*
Substances
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Anti-Bacterial Agents
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Azo Compounds
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Hydrocarbons, Aromatic
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Quinolines
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Sulfhydryl Compounds