Abstract
Pursuing our searches on quinolonecarboxylic acids we used a simple three-step one pot procedure to synthesize novel 1,7-disubstituted-6-nitroquinolones. The new derivatives were tested against Mycobacterium tuberculosis and Mycobacterium avium complex (MAC) as well as against both gram-positive and gram-negative bacteria. In vitro assays showed some derivatives were endowed with good inhibiting activities against tested mycobacteria. Some derivatives were also found more potent than ciprofloxacin and ofloxacin (used as reference drugs) against gram-positive bacteria.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / pharmacology*
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Anti-Bacterial Agents / therapeutic use
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Cell Line
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Chemistry, Pharmaceutical / methods
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Chemistry, Pharmaceutical / trends
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Ciprofloxacin / pharmacology
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Drug Evaluation, Preclinical / methods
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Fluoroquinolones / chemical synthesis*
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Fluoroquinolones / pharmacology
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Fluoroquinolones / therapeutic use
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Italy
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Microbial Sensitivity Tests / methods
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Molecular Structure
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Mycobacterium avium Complex / drug effects
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Mycobacterium tuberculosis / drug effects
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Nitroquinolines / chemical synthesis*
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Nitroquinolines / pharmacology
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Ofloxacin / pharmacology
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Fluoroquinolones
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Nitroquinolines
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Ciprofloxacin
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Ofloxacin