1-烷基-6-氟-1,4-二氢-7-(4-酰基-1-哌嗪基)-4-氧代喹啉-3-羧酸类似物的合成及其抗菌活性

Syntheses and antibacterial activity of 1-alkyl-6-fluoro-7-(4-acyl-1-piperazinyl)-1,4-dihydro-4-oxo- quinoline-3-carboxylic acid and its derivatives

目的设计合成具有广谱抗菌活性的含氟喹诺酮类化合物。方法利用吡酮酸 7位哌嗪基 4位氮上存在的活性氢为反应修饰基点 ,与磺酰氯 ,酰氯 ,氯甲酸酯进行Schotten Baumann酰基化反应设计合成一系列含有磺酰基、酰基和烷氧羰基类氟喹诺酮类似物。结果合成了 2 0个含有磺酰基、酰基和烷氧羰基的氟喹诺酮类似物 ,利用元素分析、核磁共振进行了结构确认。结论合成了16个未见报道的新化合物 ,初步体外活性测试结果表明 ,其中的 4个化合物有较高的生物活性。

Aim To synthesize new fluoroquinolone analogues as antibacterials.Methods By the reaction of the fluoroquinolone analogues with chlorides of the acid,the chloro carbonic ester under the condition of Schotten Baumann,20 fluoroquinolone analogues,including 16 new compounds were prepared.Results The structures of the synthesized compounds were determined by 1H NMR and elementary analysis.Inhibiting activity in vitro was tested.Conclusion The 16 compounds prepared were new compounds and 4 of them showed higher activity than those of the compared compound.