Abstract
We synthesized a diverse series of 9H-isothiazolo[5,4-b]quinoline-3,4-diones containing heteroaromatic groups at the 7-position via palladium-catalyzed cross-coupling. Many of these compounds demonstrated potent antistaphylococcal activity (MICs 2 microg/mL) against a multi-drug-resistant strain (ATCC 700699) and low cytotoxic activity (CC(50)>100 microM) against the human cell line Hep2 (laryngeal carcinoma).
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, Tumor
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Cyclization
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Fluorine / chemistry
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Humans
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Methicillin Resistance*
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Molecular Structure
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Quinolones / chemical synthesis
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Quinolones / chemistry
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Quinolones / pharmacology*
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Quinolones / toxicity
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / physiology
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Structure-Activity Relationship
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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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Quinolones
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Sulfhydryl Compounds
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Fluorine