Synthesis of 7-substituted-1-substituted-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolonecarboxylic acid compounds and their antibacterial activity in vitro / 第二军医大学学报

ABSTRACT

Objective: To study the synthesis, antibacterial activities and structure activity relationship of 7 substituted 1 substituted 6,8 difluoro 1,4 dihydro 4 oxo 3 quinolonecarboxylic acid compounds. Methods: The title compounds were synthesized through the process of condensation, Gould Jacobs cyclization, nucleophilic substitution. Antibacterial activities in vitro were determined with 10 kinds of common pathogenic bacteria. Results: Twenty six compounds of 7 substituted 1 substituted 6,8 difluoro 1,4 dihydro 4 oxo 3 quinolonecarboxylic acids were designed and synthesized. Among them 20 compounds were firstly reported. The chemical structures of all the compounds were determined by IR, 1HNMR and elementary analysis. Especially for type Ⅲ, compound Ⅲ b2 had more potent activity compared with fleroxacin in vitro . Conclusion: Among the 26 kinds of compounds synthesized, some of them have good antibacterial activities, the antibacterial activity of compound Ⅲ b2 is better than fleroracin. The compounds of type Ⅲ should be further studied.