1-取代苄基喹啉酮酸衍生物的合成与抗菌活性

喹啉酮酸类化合物是近年来研究发展十分迅速的广谱、高效、低毒的抗菌药物。作者合成并测定了近三十个6-氟-7-取代氨基取代的1-取代苄基喹啉酮酸类化合物,对金黄色葡萄球菌25923,大肠杆菌25922以及绿脓杆菌的MIC(μg/ml)值。结果表明,这类化合物的体外抗菌活性均较低,对革兰氏阳性菌的作用相对强于对革兰氏阴性菌的作用。1-取代苄基抗菌活性顺序一般为:苄基>对氯苄基>对硝基苄基。

Synthesis and antibacterial activity of 1-substituted benzyl quinolone acid derivatives

The compounds of quinolone class, which were studied extensively and developed very quickly in the last decades, showed high activity, low toxicity and broad antibacterial spectrum. About thirty new compounds of 1,7-disubstituted-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acids were synthesised and evaluated in vitro against S. aureus 25923, E. coli-25922 and P. aeruginosa. Their activities were low. The minimum inhibitory concentrations (MIC microgram/ml) of these compounds against Gram-positive bacteria were higher than those against Gram-negative bacteria. The relative in vitro activity contributed by 1-benzyl was: benzyl greater than p-chlorobenzyl greater than p-nitrobenzyl groups.