Nitroquinolones with broad-spectrum antimycobacterial activity in vitro. |
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Authors: | M Artico A Mai G Sbardella S Massa C Musiu S Lostia F Demontis P La Colla |
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Affiliation: | Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Italy. artico@uniromal.it |
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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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