吡酮酸类抗菌药物的研究Ⅶ.1-对氟苯基-6-氟-1,4-二氢-4-氧-7-取代-吡啶[2,3-C]并哒嗪-3-羧酸的合成和抗菌活性

STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS VII.SYNTHESIS ANDANTIBACTERIAL ACTIVITIES OF 1-(P-FLUOROPHENYL)-6-FLUORO-1,4-DIHYDRO-4-OXO-7-SUBSTITUTED PYRIDINO (2,3-C)PYRIDAZIN-3-DABOXYLIC ACIDS

为研究吡酮酸类化合物的构效关系,设计合成了1-对氟苯基-6-氟-1,4-二氢-4-氧-7-取代-吡啶[2,3-C]并哒嗪-3-羧酸(19)～(32),并测定了它们的体外抗菌活性。化合物(19)～(32)对E.coli1515的最低抑菌浓度均大于或等于100μg/ml。

L-(P-fluorophenyl)-6-fluoro-l, 4-dihydro-4-oxo-7-substituted pyr dino (2,3-C-)pyridazin-3-carboxylic acids were designed and prepared for the study of the structure activity relationship. The antibacterial activites in vitro of thesecomp-ounds were tested. Compounds 19-32 showed MIC against E. coli 1515 at100μ/ml.