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  • Title: Pyridonecarboxylic acids as antibacterial agents. VI. Synthesis and structure-activity relationship of 7-(alkyl, cycloalkyl, and vinyl)-1-cyclopropyl-6-fluoro-4-quinolone-3-carboxylic acids.
    Author: Todo Y, Takagi H, Iino F, Fukuoka Y, Ikeda Y, Tanaka K, Saikawa I, Narita H.
    Journal: Chem Pharm Bull (Tokyo); 1994 Oct; 42(10):2049-54. PubMed ID: 7805129.
    Abstract:
    The title compounds (1a-i) have been synthesized starting with ethyl 1-cyclopropyl-6,7-difluoro-4-quinolone-3-carboxylate (2). The 7-cyclopropyl and 7-vinyl derivative (1e and 1i) exhibited potent in vitro antibacterial activities against both gram-positive and gram-negative bacteria, being equipotent with ciprofloxacin (CPFX) except for the activity against Pseudomonas aeruginosa. The two compounds were significantly less toxic than CPFX in terms of convulsion-induction as determined by intracerebral administration to mice, but showed lower urinary recoveries on intravenous administration.
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