The invention discloses a chirality 7-(piperazine-substituted pyrazol aldehyde condensation isoniazide) fluoroquinolone carboxylic acid derivative as well as a preparation method and application thereof. The chirality 7-(piperazine-substituted pyrazol aldehyde condensation isoniazide) fluoroquinolone carboxylic acid derivative is a compound with the general structural formula (I), wherein R1 is H, methyl or ethyl, and R2 is H or methyl. According to the chirality 7-(piperazine-substituted pyrazol aldehyde condensation isoniazide) fluoroquinolone carboxylic acid derivative provided by the invention, fluoroquinolone, isoniazide and pyrazole aldehyde hydrazone are effectively combined to form a compound with a new structure; superposition and cooperation of activity are achieved; superposition of the three pharmacophores of fluoroquinolone, isoniazide and pyrazole aldehyde hydrazone is realized, the antituberculosis activity is improved, the toxic and side effects of fluoroquinolone and isoniazide to normal cells are decreased, and meanwhile, the probability that mycobacterium tuberculosis resists such drugs can be lowered; the chirality 7-(piperazine-substituted pyrazol aldehyde condensation isoniazide) fluoroquinolone carboxylic acid derivative can serve as an antituberculous active substance used for development of an antituberculous drug with a new structure.