Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropyl-quinolone derivative
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 i...
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| Published in: | Journal of medicinal chemistry Vol. 31; no. 9; pp. 1694 - 1798 |
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| Main Authors: | , , , |
| Format: | Journal Article |
| Language: | English |
| Published: |
01-01-1988
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| Online Access: | Get full text |
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| Summary: | 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. |
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| Bibliography: | ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 content type line 23 |
| ISSN: | 0022-2623 |