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.
出处
《华西药学杂志》
CAS
CSCD
北大核心
2010年第3期253-256,共4页
West China Journal of Pharmaceutical Sciences
关键词
喹诺酮
顺反异构
环己烷
合成
抗菌活性
Quinolone
Cis-
trans-isomerism
Cyclohexane
Synthesis
Antibacterial effect