Abstract
A novel conformationally restricted 1-cyclopropylquinolone (1) that incorporates structural features of both ofloxacin and ciprofloxacin has been prepared. Compound 1 was found to be a DNA gyrase inhibitor having potency similar to ofloxacin but less than ciprofloxacin. The cellular inhibitory and in vivo antibacterial potencies of 1 were found to be less than those of the two reference agents.
MeSH terms
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Animals
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Bacteroides / enzymology
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Chemical Phenomena
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Chemistry
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Ciprofloxacin / pharmacology
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Escherichia coli / enzymology
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Mice
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Ofloxacin
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Oxazines / chemical synthesis
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Oxazines / pharmacology*
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Pseudomonas aeruginosa / enzymology
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Staphylococcus aureus / enzymology
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Streptococcus / enzymology
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Topoisomerase II Inhibitors*
Substances
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Oxazines
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Topoisomerase II Inhibitors
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9'-fluoro-10'-(4-methyl-1-piperazinyl)-7'-oxospiro(cyclopropane-1,3'(2'H)-(7H)pyrido(1,2,3-de)(1,4)benzoxazine)-6'-carboxylic acid
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Ciprofloxacin
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Ofloxacin