Comparative study of new benzenesulphonamide fluoroquinolones structurally related to ciprofloxacin against selected ciprofloxacin-susceptible and -resistant Gram-positive cocci.
The in vitro activities of benzenesulphonamide fluoroquinolones (BSFQs) I-III, new fluoroquinolones with a p-substituted benzenesulphonyl moiety attached to the C(7) piperazinyl ring of ciprofloxacin, were assessed in comparison with those of N-sulfanilylpiperazinyl fluoroquinolone (NSFQ)-105 and ciprofloxacin for 133 Gram-positive clinical isolates. NSFQ-105 and BSFQ-I were the most active drugs. They were 16- to 64-fold more active than ciprofloxacin against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, including ciprofloxacin-resistant strains, and Streptococcus pneumoniae (eight- to 32-fold). A high degree of correlation was found between the MICs of the new compounds and ciprofloxacin for Staphylococcus spp. and E. faecalis. Staphylococci and enterococci exhibit cross-resistance to BSFQs and ciprofloxacin.
Alovero
F
F
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, (5000) Ciudad Universitaria, Córdoba, Argentina.
Barnes
A
A
Nieto
M
M
Mazzieri
M R
MR
Manzo
R H
RH
D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000031:analogs & derivatives / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D006095:Gram-Positive Cocci / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D000096926:Benzenesulfonamides
D000890:Anti-Infective Agents; D002939:Ciprofloxacin; D013449:Sulfonamides; D000096926:Benzenesulfonamides