Benzenecarboxamide Analogs of Fluoroquinolones (BCFQs). Antibacterial Activity and SAR Studies

The bioisosteric replacement of the sulfonyl group, in the previously reported benzenesulfonylamidofluoroquinolones (BSFQs), for a carbonyl group was the principle that led to the design of benzenecarboxamide fluoroquinolones (BCFQs). Six new derivatives were prepared and tested against Grampositive and -negative bacteria. As a result, the activity against Staphylococcus aureus of the new series was comparable with norfloxacin or ciprofloxacin but decreased when compared with BSFQs. These findings are significant since the new BCFQs could be incorporated into the selected family of "dual targeting" AMFQs.