In vitro and in vivo antibacterial activities of DW286, a new fluoronaphthyridone antibiotic.
The in vitro and in vivo activities of DW286, a novel fluoronaphthyridone with potent antibacterial activity, were compared with those of ciprofloxacin, gemifloxacin, sparfloxacin, and trovafloxacin. Against gram-positive bacteria, such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Enterococcus faecalis, the in vitro activity of DW286 was stronger than that of any other reference antibiotic. Against gram-negative bacteria, the activity of DW286 was similar to those of trovafloxacin and gemifloxacin but was weaker than that of ciprofloxacin. In a mouse systemic infection caused by three S. aureus strains, including methicillin-resistant S. aureus and quinolone-resistant S. aureus (QRSA), DW286 demonstrated the most potent activity, as found in vitro. Specially, DW286 is >or=8-fold more active against QRSA than the other fluoroquinolones. And the 50% protective doses for DW286 were correspondent with the in vitro activities.
Yun
Hee-Jeong
HJ
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Korea.
Min
Yu-Hong
YH
Lim
Jung-A
JA
Kang
Jin-Wook
JW
Kim
So-Young
SY
Kim
Mi-Jeong
MJ
Jeong
Jae-Hee
JH
Choi
Yun-Jeong
YJ
Kwon
Hyun-Jin
HJ
Jung
Yong-Ho
YH
Shim
Mi-Ja
MJ
Choi
Eung-Chil
EC
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D000890:Anti-Infective Agents / Q000494:pharmacology / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D004285:Dogs; D024841:Fluoroquinolones; D051379:Mice; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000494:pharmacology*; D051381:Rats
C471029:7-(3-(aminomethyl)-4-(methoxyimino)-3-methyltetrahydro-1H-1-pyrrolyl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro(1,8)naphthyridine-3-carboxylic acid; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines