| 摘要 |
PURPOSE: Novel quinolonecarboxylic acid derivatives are provided which have a broad antibacterial spectrum and an excellent antibacterial activity and which show significantly excellent pharmacodynamic properties. And their pharmaceutically acceptable salts, esters, solvates and isomers are provided. Also, their preparation method and an antibacterial composition comprising the compounds as an effective ingredient are provided. CONSTITUTION: The novel quinolonecarboxylic acid derivatives, which have (4-aminomethyl-3-substituted oxime-2-methyl) pyrrolidine group at the position 7 of a quinolone mother nucleus, are represented by the formula (1), wherein: R1 is C1-C5 alkyl, C3-C6 cycloalkyl or dihalophenyl; R2 is hydrogen, C1-C5 alkyl or amino; Q is C-H, C-F, C-Cl, C-CH3, C-O-CH3 or N; R3 is C1-C5 alkyl, C3-C6 cycloalkyl, C3-C6 cycloalkyl C1-C5 alkyl, C3-C6 alkenyl, C3-C6 alkynyl, C1-C5 haloalkyl, or substituted or unsubstituted phenyl or benzyl. A method for preparing the derivatives is characterized by comprising the step of reacting the compound of formula (2) with the compound of formula (3) in a solvent, in the presence of base. In the formulae (2) and (3), R1, R2, R3 and Q are as defined above, and X represents halogen.
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