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  • Title: Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
    Author: Artico M, Mai A, Sbardella G, Massa S, Musiu C, Lostia S, Demontis F, La Colla P.
    Journal: Bioorg Med Chem Lett; 1999 Jun 21; 9(12):1651-6. PubMed ID: 10397494.
    Abstract:
    During search on quinolonecarboxylic acids we used a facile, convenient two- or three-step procedure to synthesize new quinolone analogs, bearing at the C-7 position alkylamino substituents, and at the C-6 position a fluorine or alternatively a nitro group. The new derivatives were tested against both Gram-positive and Gram-negative bacteria and against a number of different mycobacteria. In vitro assays showed 1-tert-butyl-7-tert-butylamino-6-nitro-1,4-dihydro-4-quinolone-3-carboxy lic acid to be a potent inhibitor of Streptococcus and Staphylococcus with potencies superior to those of ofloxacin and ciprofloxacin, used as reference drugs. Some 6-nitroquinolones were found to exert good inhibiting activities against Mycobacterium tuberculosis and various atypical mycobacteria, whereas the 6-fluoro counterparts showed poor or no activity against this bacterium.
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