88569-33-9Relevant academic research and scientific papers
1-Amino (or substituted amino)-1,4-dihydro-4-oxo-6-fluoro-7-heterylquinoline-3-carboxylic acids and their use as antibacterial agents
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, (2008/06/13)
Novel 1-R-1,4-dihydro-4-oxo-6-fluoro-7-(Z=N--)-quinolinecarboxylic acids and esters thereof, where R is amino, lower-alkylamino, 2-propenylamino or di-lower-alkylamino, R" is hydrogen or lower-alkyl, and Z=N is a heterocyclic group, useful as antibacterial agents, are prepared by reacting the corresponding 7-chloroquinoline derivatives with the appropriate heterocyclic compound, Z=NH. A preferred group of compounds are those where Z=N is 1-piperazinyl or 4-lower-alkyl-1-piperazinyl.
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: Synthesis and structure-activity relationships
Wentland,Bailey,Cornett,Dobson,Powles,Wagner
, p. 1103 - 1108 (2007/10/02)
A series of novel 3-quinolinecarboxylic acid derivatives have been prepared and their antibacterial activity evaluated. These derivatives are characterized by fluorine attached to the 6-position and substituted amino groups appended to the 1- and 7-positions. Structure-activity relationship studies indicate that antibacterial potency is greatest when the 1-substituent is methylamino and the 7-substituent is either 4-methyl-1-piperazinyl, 16, or 1-piperazinyl, 21. Derivatives 16 and 21, the 1-methylamino analogues of pefloxacin and norfloxacin, respectively, show comparable in vitro and in vivo antibacterial potency to these two known agents. The activity (vs Escherichia coli Vogel) of 16 (amifloxacin) is the following: in vitro MIC (μg/mL) = 0.25; in vivo (mice) PD50 (mg/kg) = 1.0 (po), 0.6 (sc).
