[In vitro antibacterial activity of prulifloxacin, a new oral fluoroquinolone].
We compared antibacterial activity of NM394, which is the active metabolite of a prodrug of new fluoroquinolone prulifloxacin (PUFX), against clinical isolates of bacteria with those of ciprofloxacin (CPFX), levofloxacin (LVFX), gatifloxacin (GFLX), tosufloxacin (TFLX) and fleroxacin (FLRX). 1. NM394 showed a broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria. 2. MIC80 of NM394 for methicillin-sensitive Staphylococcus aureus, Streptococcus pneumoniae and Enterococcus faecalis were 0.5 microgram/ml, 2 micrograms/ml and 4 micrograms/ml, respectively. MIC80 of NM394 for Escherichia coli, Klebsiella pneumoniae and Enterobacter cloacae was lower than 0.06 microgram/ml. MIC80 of NM394 for Serratia marcescens and Pseudomonas aeruginosa were 0.25 microgram/ml and 2 micrograms/ml, respectively. 3. Short-time bactericidal activity of NM394 against P. aeruginosa was stronger than those of CPFX, GFLX, LVFX and TFLX. 4. Short-time bactericidal activity of NM394 at Cmax concentration against 12 strains of P. aeruginosa was stronger than those of CPFX, LVFX, GFLX and TFLX.
Araake
Minako
M
Department of Microbiology, Kyoto Pharmaceutical University.
Hara
Tetsuro
T
Watabe
Hiroomi
H
Nishino
Takeshi
T
D000890:Anti-Infective Agents / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000494:pharmacology; D004148:Dioxolanes / Q000494:pharmacology*; D004304:Dosage Forms; D004305:Dose-Response Relationship, Drug; D024881:Drug Resistance, Bacterial; D016576:Fleroxacin / Q000494:pharmacology; D024841:Fluoroquinolones; D000077734:Gatifloxacin; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000302:isolation & purification; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D064704:Levofloxacin; D009287:Naphthyridines / Q000494:pharmacology; D015242:Ofloxacin / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology*; D011355:Prodrugs / Q000494:pharmacology*; D015363:Quinolones / Q000494:pharmacology*
D000890:Anti-Infective Agents; D004148:Dioxolanes; D004304:Dosage Forms; D024841:Fluoroquinolones; D009287:Naphthyridines; D010879:Piperazines; D011355:Prodrugs; D015363:Quinolones; D002939:Ciprofloxacin; D064704:Levofloxacin; D015242:Ofloxacin; C074190:ulifloxacin; C055185:tosufloxacin; C074191:prulifloxacin; D000077734:Gatifloxacin; D016576:Fleroxacin