Quinolonecarboxylic acid derivatives and their preparation.

摘要

Quinolonecarboxylic acid derivatives of the following formu­la,
<Chemistry id="chema01" num="0001"><Image id="ia01" he="34" wi="67" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> wherein R indicates straight or branched lower alkyl, R¹ indi­cates cycloalkyl having 3 to 6 carbon atoms, straight or branched lower alkyl, halogenoalkyl, alkenyl, hydroxyalkyl, lower alkyl­amino or substituted or non-substituted phenyl, R² indicates hydrogen, halogen, nitro or amino, X indicates halogen, Z indi­cates halogen, azetidino, pyrrolidino, piperidino, morpholino, thiomorpholino, piperazino or homopiperazino of the following formula,
<Chemistry id="chema02" num="0002"><Image id="ia02" he="26" wi="58" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> (here, n is 1 or 2, R³ indicated hydrogen, lower alkyl, lower acyl, acyloxycarbonyl or benzyl, R⁴ and R⁵ indicate hydrogen, lower alkyl, aminoalkyl, hydroxyalkyl or phenyl each independent­ly), or pyrrolidino or piperidino of the following formula,
<Chemistry id="chema03" num="0003"><Image id="ia03" he="21" wi="66" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> (here, k is 0, 1 or 2, l is 0, 1 or 2, m is 0 or 1, R⁶ indicates hydrogen, lower alkyl or hydroxy, R⁷ indicates hydrogen, lower alkyl, halogenoalkyl or hydroxyalkyl, R⁸ indicates hydrogen, lower alkyl, lower acyl, alkoxycarbonyl or benzyl), the hydrates and pharmaceutically acceptable acid addition or alkali salts thereof are useful as antibacterial agents.