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  • Title: Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride.
    Author: Chu DT, Nordeen CW, Hardy DJ, Swanson RN, Giardina WJ, Pernet AG, Plattner JJ.
    Journal: J Med Chem; 1991 Jan; 34(1):168-74. PubMed ID: 1846917.
    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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