title: In vitro activity of BAY 12-8039, a new fluoroquinolone, against species representative of respiratory tract pathogens.
abstract: The in vitro antibacterial activity of BAY 12-8039, a novel 8-methoxy-quinolone, was compared with those of other quinolones, amoxicillin/clavulanate, cefuroxime and erythromycin against species commonly implicated in respiratory tract infections as well as viridans group streptococci. The new compound was highly active against methicillin-susceptible staphylococci (MIC90 0.125 microgram/ml), penicillin-susceptible and penicillin-resistant pneumococci (MIC90 0.5 and MIC50 0.25 microgram/ml, respectively), penicillin-susceptible and penicillin-resistant viridans group streptococci (MIC90 0.5 and 0.25 microgram/ml, respectively), group A streptococci (MIC90 0.25 microgram/ml), M. catarrhalis (MIC90 0.125 microgram/ml) and H. influenzae (MIC90 0.063 microgram/ml), irrespective of beta-lactamase production. It was, however, less active against methicillin-resistant staphylococci (MIC50 and MIC90, 2 and 4 micrograms/ml, respectively). The new compound demonstrated bactericidal activity at concentrations 2, 4, 8 times the MIC against representative isolates of the above collection. At a concentration of eight times the MIC, the frequency of spontaneous resistance ranged from 2.5 x 10(-7) to < 4 x 10(-8). These results suggested that BAY 12-8039 would be a promising agent for the eradication of respiratory tract pathogens and that clinical trials assessing its efficacy for the management of infections caused by these organisms are warranted.
authors.affiliation: Department of Medicine, Beth Israel Deaconess Medical Center, Boston, MA 02115, USA.
authors.forename: M
authors.initials: M
authors.lastname: Souli
authors.forename: C B
authors.initials: CB
authors.lastname: Wennersten
authors.forename: G M
authors.initials: GM
authors.lastname: Eliopoulos
mesh_terms: D000658:Amoxicillin / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000494:pharmacology*; D001372:Aza Compounds; D002444:Cefuroxime / Q000494:pharmacology; D019818:Clavulanic Acid / Q000494:pharmacology; D004917:Erythromycin / Q000494:pharmacology; D024841:Fluoroquinolones; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D001936:Moraxella catarrhalis / Q000187:drug effects; D000077266:Moxifloxacin; D010403:Penicillin Resistance; D011804:Quinolines; D015363:Quinolones / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013291:Streptococcus / Q000187:drug effects*; D013296:Streptococcus pneumoniae / Q000187:drug effects*; D013297:Streptococcus pyogenes / Q000187:drug effects
chemical_list: D000890:Anti-Infective Agents; D001372:Aza Compounds; D024841:Fluoroquinolones; D011804:Quinolines; D015363:Quinolones; D019818:Clavulanic Acid; D004917:Erythromycin; D000658:Amoxicillin; D002444:Cefuroxime; D000077266:Moxifloxacin