摘要
通过5-氨基-1-环丙基-6,7-二氟-8-甲氧基-1,4-二氢-4-氧代喹啉-3-羧酸与不同的环胺进行缩合反应,合成了5个未见文献报道的5-氨基-8-甲氧基喹诺酮类化合物。它们的结构均经核磁共振氢谱和高分辨质谱所确证。用环丙沙星及加替沙星作对照,测定了它们的体外抗菌活性,结果表明它们具有广谱活性,其中化合物5、7和9活性十分明显地优于对照药;化合物5和9进一步评价了其体内活性,结果表明化合物5和9分别比对照药加替沙星和莫西沙星具有更优秀的体内活性,值得深入研究。
Five compounds of 7-substitued-l-cyclopropyl-5-amino-6-fluoro-8-methoxyquinoline-3-car- boxylic acids have been prepared and evaluated for the antibacterial activities in vitro and in vivo. From results compounds 5 and 9 have more higher activity than gatifloxacin and moxifloxacin. On the basis of these results, compounds 5 and 9 were selected as candidates for further evaluation.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2007年第12期754-756,764,共4页
Chinese Journal of Antibiotics
关键词
喹诺酮
合成
抗菌作用
Quinolone
Synthesis
Antibacterial activity
