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含硫三环氟喹诺酮类化合物的合成及其抗菌活性研究
引用本文:王秀珍,王尔华.含硫三环氟喹诺酮类化合物的合成及其抗菌活性研究[J].药学进展,2004,28(11):502-507.
作者姓名:王秀珍  王尔华
作者单位:1. 南京医科大学药化教研室,江苏,南京,210029
2. 中国药科大学医药化工研究所,江苏,南京,210009
摘    要:目的:寻找具有更好抗菌活性的含硫三环氟喹诺酮类化合物。方法:在芦氟沙星母核的10位引入不同基团,设计并合成8个含硫三环氟喹诺酮类化合物,并测定其体外抗菌活性。结果:合成了目标化合物,其结构经IR、^1HNMR、MS和元素分析确证;它们具有不同强度的抗菌活性,其中几个化合物的抗菌活性优于芦氟沙星。结论:初步的体外抗菌实验证实所合成目标化合物具明显的抗菌活性,甚至优于芦氟沙星。

关 键 词:含硫三环氟喹诺酮  芦氟沙星  合成  抗菌活性
文章编号:1001-5094(2004)11-0502-06
修稿时间:2004年7月28日

Synthesis and Antibacterial Activity of Sulfur-containing Tricyclic Fluoroquinolones
WANG Xiu-zhen ,WANG Er-hua.Synthesis and Antibacterial Activity of Sulfur-containing Tricyclic Fluoroquinolones[J].Progress in Pharmaceutical Sciences,2004,28(11):502-507.
Authors:WANG Xiu-zhen  WANG Er-hua
Institution:WANG Xiu-zhen 1,WANG Er-hua 2*
Abstract:Obstract: To search for nov el sulfur-containing tricyclic fluoroquinolone compounds with better antibacteria l activity. Methods: Different groups were introduced into the t enth position of rufloxacin parent structure, thus 8 sulfur-containing tricycli c fluoroquinolones were synthesized. And their in vitro antibacterial activities were evaluated by MICs against a variety of bacteria. Results: The target compounds were synthesized, their structures were confirmed by 1 HNMR, MS, IR spectra and elementary analysis and they showed different powers in antibacterial activity, of which some had higher activity than that of ruflox acin. Conclusion: The results of preliminary antibacterial activity test showed that the target compounds had antibacterial activity to different degree .
Keywords:Sulfur-containing tricyclic fluoroquinolone  Ruf loxacin  Synthesis  Antibacterial activity
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