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  • Title: Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
    Author: Hagen SE, Domagala JM, Heifetz CL, Johnson J.
    Journal: J Med Chem; 1991 Mar; 34(3):1155-61. PubMed ID: 2002456.
    Abstract:
    A series of 5-alkyl-1,7,8-trisubstituted-6-fluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids was prepared and evaluated for in vitro and in vivo antibacterial activity. When compared to the 5-hydrogen analogues, the presence of the 5-methyl group enhanced in vitro potency for those compounds containing a cyclopropyl moiety at N1 but decreased potency for those containing an ethyl group at N1. Replacing the 5-methyl with a 5-ethyl significantly reduced the efficacy. In general, the 5-methyl and 5-hydrogen analogues were equipotent in vivo. Several of the 5-methyl-1-cyclopropylquinolones displayed excellent in vitro and in vivo activity, warranting further development.
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