
Journal of Medicinal Chemistry p. 168 - 174 (1991)
Update date:2022-08-03
Topics:
Chu, Daniel T. W.
Nordeen, Carl W.
Hardy, Dwight J.
Swanson, Robert N.
Giardina, William J.
et al.
Temafloxacin hydrochloride <(+/-)-7-(3-methylpiperazin-1-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride> is a potent member of the 4-pyridone-3-carboxylic acid class of antibacterial agents and is currently under clinical development as a broad-spectrum antimicrobial agent.It is a racemate having a chiral center at the C3 of the 7-piperazin-1-yl group.The two enantiomers were synthesized and tested for their antibacterial activities.Although no difference in in vitro antibacterial activities was observed, a minor difference in in vivo antibacterial activities was observed.However, they both exhibited similar pharmacological profiles.
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