ABSTRACT
The in vitro spectrum of a novel des-fluoro(6) quinolone, BMS-284756, was compared with those of five fluoroquinolones (trovafloxacin, moxifloxacin, levofloxacin, ofloxacin, and ciprofloxacin). BMS-284756 was among the most active and often was the most active quinolone against staphylococci (including methicillin-resistant strains), streptococci, pneumococci (including ciprofloxacin-nonsusceptible and penicillin-resistant strains), andEnterococcus faecalis. BMS-284756 inhibited ≈60 to ≈70% of the Enterococcus faecium (including vancomycin-resistant) strains and 90 to 100% of theEnterobacteriaceae strains and gastroenteric bacillary pathogens at the anticipated MIC susceptible breakpoint (≤4 μg/ml). Against the nonfermenters, BMS-284756 inhibited 90 to 100% ofPseudomonas fluorescens, Pseudomonas stutzeri,Stenotrophomonas maltophilia, Flavobacteriumspp., and Acinetobacter spp. and 72% ofPseudomonas aeruginosa strains at 4 μg/ml. Against anaerobic bacteria, BMS-284756 was among the most active, inhibiting essentially all strains tested. It had very low MICs against the fastidious and atypical microbial species, in particular against mycoplasmas or ureaplasmas, Borrelia burgdorferi, chlamydia, and gonococci. These results indicate that with its broad antibacterial spectrum, BMS-284756 should be evaluated clinically for the treatment of community and nosocomial infections.
Design, Synthesis, Molecular Docking and Antibacterial Screening of Some Quinolone Compounds