title: In vitro activity of sparfloxacin (CI-978, AT-4140, and PD 131501). A quinolone with high activity against gram-positive bacteria.
abstract: Sparfloxacin (CI-978, AT-4140 and PD 131501) is a new antimicrobial agent of the piperazinyl quinolone class. Relative to other quinolones, it is a potent antistaphylococcal and antistreptococcal drug in vitro: The microbroth 90% minimum inhibitory concentration (MIC90) (in microgram/ml) was 0.25 vs 26 methicillin-resistant and -sensitive coagulase-positive and -negative staphylococci and 20 Streptococcus pneumoniae; 0.5 vs 20 strains each of S. pyogenes, S. agalactiae, and Enterococcus faecalis. The data indicate sparfloxacin to be generally superior to ciprofloxacin, ofloxacin, oxacillin, cefazolin, doxycycline, amikacin, and vancomycin against these Gram-positive bacterial groups. Additional MIC90s were determined for Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, and Neisseria gonorrhoeae (less than or equal to 0.03); Enterobacteriaceae (0.5); and Listeria monocytogenes (1). Activity was generally unchanged with light, 50% human serum, aerobic-anaerobic atmosphere, 5% sodium cholate, cation supplementation, and 100-fold increased or decreased inoculum; as with other quinolones, potency was measurably diminished with decreasing pH (pH less than or equal to 6.0) and in 100% urine. Naturally occurring resistant mutants occurred at frequencies of 10(-8) or lower.
authors.affiliation: Parke-Davis Pharmaceutical Research Division, Ann Arbor, Michigan 48105.
authors.forename: M A
authors.initials: MA
authors.lastname: Cohen
authors.forename: M D
authors.initials: MD
authors.lastname: Huband
authors.forename: G B
authors.initials: GB
authors.lastname: Mailloux
authors.forename: S L
authors.initials: SL
authors.lastname: Yoder
authors.forename: G E
authors.initials: GE
authors.lastname: Roland
authors.forename: C L
authors.initials: CL
authors.lastname: Heifetz
mesh_terms: D000890:Anti-Infective Agents / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004352:Drug Resistance, Microbial; D013293:Enterococcus faecalis / Q000187:drug effects; D024841:Fluoroquinolones; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D009154:Mutation; D015363:Quinolones / Q000494:pharmacology*; D013292:Streptococcus agalactiae / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; C061363:sparfloxacin