Antibacterial activities and inhibitory effects of sitafloxacin (DU-6859a) and its optical isomers against type II topoisomerases.
The in vitro inhibitory effects of sitafloxacin (DU-6859a) and its three stereoisomers on bacterial DNA gyrase from Escherichia coli, topoisomerase IV from Staphylococcus aureus, and topoisomerase II from human placenta were compared. No correlation was observed between the inhibitory activities of quinolones against bacterial type II topoisomerases and those against human topoisomerase II. Sitafloxacin showed the most potent inhibitory activities against bacterial type II topoisomerases and the lowest activity against human type II topoisomerase.
Akasaka
T
T
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan. XLX06563@niftyserve.or.jp
Kurosaka
S
S
Uchida
Y
Y
Tanaka
M
M
Sato
K
K
Hayakawa
I
I
D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000187:drug effects; D027101:DNA Topoisomerase IV; D004250:DNA Topoisomerases, Type II / Q000187:drug effects*; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D024841:Fluoroquinolones; D006801:Humans; D008826:Microbial Sensitivity Tests; D010920:Placenta / Q000187:drug effects / Q000201:enzymology; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000201:enzymology; D013237:Stereoisomerism
D000890:Anti-Infective Agents; D001426:Bacterial Proteins; D024841:Fluoroquinolones; D015363:Quinolones; C076246:sitafloxacin; D027101:DNA Topoisomerase IV; D004250:DNA Topoisomerases, Type II