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KMID : 0043319960190010052
Archives of Pharmacal Research
1996 Volume.19 No. 1 p.52 ~ p.59
In vitro Activities of LB20304, a New Fluoroquinolone
Kim Mu-Yong

Oh Jeong-In
Paek Kyoung-Sook
Hong Chang-Yong
Kim In-Chull
Kwak Jin-Hwan
Abstract
The in vitro activity of LB20304 was evaluated against clinical isolates and compared with those of Q-35, ciprofloxacin, sparfloxacin, lomefloxacin and ofloxacin. LB20304 demonstrated 16-to 64-fold more potent activity than ciprofloxacin against gram-positive bacteria. LB20304 inhibited 90% of the isolates of methicillin-susceptible Staphylococcus aureus(MSSA) at a concentration of values of LB20304 against methicillin-resistant Staphylococcus aureus (MRSA), methicillin-susceptible Staphylococcus epidermidis (MSSE), methicillin-resistant S. epidermidis (MRSE) and Streptococcus pneumoniae were respectively. LB20304 was also very active against gram-negative bacteria. Against Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Pseudomonas aeruginosa and Acinetobacter calcoaceticus, , respectively. Its activity was comparable to that of ciprofloxacin but much better than those of Q-35, sparfloxacin, ofloxacin and lomefloxacin. LB20304 also exhibited the most potent acitvity among quinolones tested against laboratory standard strains, ofloxacin-resistant strains, .betha.-lactamase-producing strains and anaerobic strains. The inhibitory effect of LB20304 on DNA gyrase from Micrococcus luteus, determined by the supercoiling assay, was 8-fold more potent than that of ciprofloxacin. LB20304 did not induce topoisomerase-associated DNA cleavage even at a concentration of 10 mg/ml, although ciprofloxacin induced DNA cleavage at a concentration of 1 mg/ml.
KEYWORD
LB20304, Quinolone, MIC, DNA gyrase, Topoisomerase
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