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  • Title: The synthesis and antibacterial activities of quinolones containing five- and six-membered heterocyclic substituents at the 7-position.
    Author: Cooper CS, Klock PL, Chu DT, Fernandes PB.
    Journal: J Med Chem; 1990 Apr; 33(4):1246-52. PubMed ID: 2319566.
    Abstract:
    A series of 6-fluoro-7-substituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids were prepared. The substituents at the 7-position included five- and six-membered heterocyclic rings such as oxazoline and oxazine as well as five-membered heteroaromatic rings such as oxazoles and imidazoles. The structure--activity relationships (SAR) of these compounds indicated that oxazole substituents containing a 2-methyl group had the greatest in vitro potency. The compounds showed greater in vitro antibacterial activity against Gram-positive organisms than against Gram-negative organisms.
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