Trains for macrolides, from 0.12 to 0.06 with MIC90s g / ml have macrolide-resistant St Mme point mutations in the cathedral Domain V of the VOL. 47, XL880 Foretinib GSK1363089 2003 in vitro activity t of ABT 492 23S rRNA at residue 3265 corresponds to positions 2058 and 2059 in E. coli, to reduce the level of binding of the ribosomes macrolides. Although ABT 492 was two to four times a st Stronger than trovafloxacin, levofloxacin and ciprofloxacin against M. avium, all four were weakly active compounds in vitro. ABT 492 was four times st Stronger than levofloxacin and ciprofloxacin against M. pneumoniae, with an MIC90 of 0.5 g / ml, but trovafloxacin was twice as potent as ABT 492nd Chlamydia spp. obligate intracellular rer bacteria, and methods for susceptibility testing require the use of infected S mammalian cells.
The MIC of ABT 492 ABT-751 for two St Strains of C. trachomatis in this study were 0.03 and 0.06 g / ml, which were comparable to the MIC of trovafloxacin, w While levofloxacin and ciprofloxacin were less active. These results show that ABT 492 accumulates and retains antibacterial activity lt t in S Ugetierzellen. Anaerobes. Early quinolones such as ciprofloxacin typically had in vitro activity T points against anaerobic species poor, however, that improved the potency and trovafloxacin for the treatment of infections caused by anaerobes indicated. In vitro activity of ABT 492 t was at least 10 times the trovafloxacin against trovafloxacin-susceptible isolates of three species of anaerobic bacteria: the MIC 90 of ABT 492 was 0.
12 g / ml for Bacteroides fragilis and was less than 0 , 03 g / ml of Clostridium perfringens and Clostridium difficile. Levofloxacin and ciprofloxacin were less active than ABT 492 and trovafloxacin. The bactericidal effect. The MIC of ABT 492 were compared with the MBC for examples of Gram-positive and Gram-negative bacteria by microdilution method. ABT 492 demonstrated potent bactericidal activity of t, since the CMB were less than 0.12 g / ml and not more than four hours time Higher than the corresponding MICs for all 10 isolates. In particular, ABT 492 was bactericidal to five St Strains of S. pneumoniae, including normal isolates were resistant to quinolones, penicillin and macrolides. Ciprofloxacin is bactericidal for all isolates tested. Effect of serum on the antibacterial activity of t.
Plasma protein binding was determined as a percentage of bound drug and has been reviewed by ultracentrifugation. The results for protein binding in human plasma for trovafloxacin and ciprofloxacin are consistent with those reported in the records of the United States for these drugs, 69 and 20 to 40%. Binding protein profile of ABT 492 is similar to that of trovafloxacin: here distinctly binding in all plasma samples and a gr eren protein in the plasma of rats than in human plasma ciprofloxacin. Evaluated the effect of serum protein binding was determined by determining changes In the antibacterial activity in vitro t against St Strains of bacteria by microdilution plate. The in vitro activity Th of ABT 492 and trovafloxacin were reduced when tested on rats or 50% heatinactivated human serum have been. The effect of rat serum on the antibacterial activity of t was h Forth as human serum, the results of protein binding in parallel. Serum had little effect on the in vitro activity t of ciprofloxacin, correlated with significant