title: Mode of action of sulfanilyl fluoroquinolones.
abstract: 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.
authors.affiliation: Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Argentina.
authors.forename: F
authors.initials: F
authors.lastname: Alovero
authors.forename: M
authors.initials: M
authors.lastname: Nieto
authors.forename: M R
authors.initials: MR
authors.lastname: Mazzieri
authors.forename: R
authors.initials: R
authors.lastname: Then
authors.forename: R H
authors.initials: RH
authors.lastname: Manzo
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects*; D024841:Fluoroquinolones; D006863:Hydrogen-Ion Concentration; D008826:Microbial Sensitivity Tests; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; C091355:NSFQ-104; C091356:NSFQ-105; D015363:Quinolones