Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride. |
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| Authors: | D T Chu C W Nordeen D J Hardy R N Swanson W J Giardina A G Pernet J J Plattner |
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| Affiliation: | Anti-infective Research Division, Abbott Laboratories, Abbott Park, Illinois 60064-3500. |
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| Abstract: | 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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