Abstract
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.
Keywords: Fluoroquinolones, SAR, antimicrobial, norfloxacin, ciprofloxacin, benzenecarboxamides
Letters in Drug Design & Discovery
Title: Benzenecarboxamide Analogs of Fluoroquinolones (BCFQs). Antibacterial Activity and SAR Studies
Volume: 3 Issue: 2
Author(s): M. J. Nieto, F. L. Alovero, R. H. Manzo and M. R. Mazzieri
Affiliation:
Keywords: Fluoroquinolones, SAR, antimicrobial, norfloxacin, ciprofloxacin, benzenecarboxamides
Abstract: 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.
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Cite this article as:
Nieto J. M., Alovero L. F., Manzo H. R. and Mazzieri R. M., Benzenecarboxamide Analogs of Fluoroquinolones (BCFQs). Antibacterial Activity and SAR Studies, Letters in Drug Design & Discovery 2006; 3 (2) . https://dx.doi.org/10.2174/157018006775789702
DOI https://dx.doi.org/10.2174/157018006775789702 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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