含顺反式环己烷基元喹诺酮类衍生物的合成及抗菌活性初探  

Synthesis and preliminary antibacterial test of cis-,trans-,cyclohexane-type compounds substituted quinolone derivatives

作　　者：魏臣録 潘佳[1] 何菱[1] 齐庆蓉[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2010年第3期253-256,共4页West China Journal of Pharmaceutical Sciences

摘　　要：目的设计并合成系列含顺反式环己烷类基元的新型喹诺酮类衍生物,并探讨其活性。方法以加替沙星中间体1-环丙基-6,7-二氟-8-甲氧基-1,4-二氢-4-氧代喹啉-3-羧酸乙酯为原料,经叠氮化、氢化、酰胺化、水解,合成目标物并进行了抗菌活性的初筛。结果与结论合成了8个含顺反环己烷类基元的新型喹诺酮类化合物,结构经核磁确证;含顺式构型环己烷的化合物比相应的含反式构型环己烷的抑菌效果好。OBJECTIVE To design and synthesize a series of quinolone derivatives in order to investigate their antibacterial effect.METHODS The title compounds were synthesized from ethyl 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylate through diazotization,hydrogenation,acylation and hydrolyzation,and the preliminary antibacterial test was carried out.RESULTS and CONCLUSION The structures of these new compounds were confirmed by 1HNMR and 13CNMR.The preliminary antibacterial test suggests that cis-compounds are more effective than trans-compounds.

关 键 词：喹诺酮 顺反异构 环己烷 合成 抗菌活性 

分 类 号：R914[医药卫生—药物化学]