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Antimicrobial Agents and Chemotherapy, June 1998, p. 1495-1498, Vol. 42, No. 6
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.

Mode of Action of Sulfanilyl Fluoroquinolones

Fabiana Alovero,1 Marcelo Nieto,1 Maria Rosa Mazzieri,1 Rudolf Then,2 and Ruben H. Manzo1,*

Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina,1 and Pharma Division, Preclinical Research Infectious Diseases, F. Hoffman-La Roche Ltd., Basel, Switzerland2

Received 15 April 1997/Returned for modification 30 May 1997/Accepted 17 March 1998

The mode of action of sulfanilyl fluoroquinolones (NSFQs) was investigated with NSFQ-104, NSFQ-105, and some structurally related compounds. Evidence arising from interactions with p-aminobenzoic acid and trimethoprim suggested that a sulfonamidelike mechanism of action makes little or no contribution to the in vitro activity of NSFQs. NSFQ-105 showed an activity that inhibits gyrase-catalyzed DNA supercoiling that is similar to the activity of other fluoroquinolones. Also, NSFQ-105 uptake was decreased by the presence of Mg2+ and increased by a lower pH. These results indicate that NSFQs having only one ionizable group could exhibit more favorable kinetics of access to the bacterial cell than zwitterionic fluoroquinolones.

* Corresponding author. Mailing address: Departamento de Farmacia, Facultad de Ciencias Químicas, U.N.C. A.P. 4-C.C.61-(5000) Córdoba, Argentina. Phone: 54-51-334163. Fax: 54-51-334127. E-mail: rubmanzo{at}dqo.fcq.unc.edu.ar.

Antimicrobial Agents and Chemotherapy, June 1998, p. 1495-1498, Vol. 42, No. 6
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.


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