| 7-[(1S,5R)-2-苄基-2,6二氮杂环(3.2.1)辛烷-6-基]喹诺酮类化合物的合成与抗菌作用 |
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| 引用本文： | 刘开湘,郭惠元.7-[(1S,5R)-2-苄基-2,6二氮杂环(3.2.1)辛烷-6-基]喹诺酮类化合物的合成与抗菌作用[J].中国抗生素杂志,2002,27(3):151-156. |
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| 作者姓名： | 刘开湘 郭惠元 |
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| 作者单位： | 中国医学科学院,中国协和医科大学,医药生物技术研究所,北京100050 |
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| 摘 要： | 以 ( 4R) 羟基 L 脯氨酸为原料 ,经十三步反应得 ( 1S ,5R) 2 苄基 2 ,6 二氮杂二环 ( 3.2 .1)辛烷二氢溴酸盐 ,以此化合物作为 7位侧链 ,合成了四个喹诺酮类化合物 ,并测定了它们对 10株革兰氏阳性菌和 6株革兰氏阴性菌的MIC值 ,结果表明 ,它们的体外抗菌作用均低于对照药加替沙星和环丙沙星。本文共合成了 2 0个化合物 ,除 2、3、4外 ,其余均为文献未见报道的新化合物 ,其结构经NMR和MS所确证。
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| 关 键 词： | 氟喹诺酮 合成 抗菌活性 |
| 文章编号： | 1001-8689(2002)03-0151-06 |
| 修稿时间： | 2001年10月22 |
Synthesis and antibacterial activity of 7-[ (1S,5R ]-2-benzyl-2,6-diazabicyclo (3.2.1) octan-6-yl ] - quinolones |
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| Liu Kai-xiang and Guo Hui yuan,quinolones$$$$,Liu Kai xiang and Guo Hui yuan.Synthesis and antibacterial activity of 7-[ (1S,5R ]-2-benzyl-2,6-diazabicyclo (3.2.1) octan-6-yl ] - quinolones[J].Chinese Journal of Antibiotics,2002,27(3):151-156. |
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| Authors: | Liu Kai-xiang and Guo Hui yuan quinolones$$$$ Liu Kai xiang and Guo Hui yuan |
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| Abstract: | S,5R) 2 benzyl 2,6 diazabicyclo (3.2.1) octane dihydrobromide was synthesized by l3 steps from trans 4 hydroxy L proline. Four quinolone derivatives was synthesized with the compound as 7 position side chain,and in vitro antibacterial activities of these quinolones were tested. Results showed that they have lower activities than those of ciprofloxacin and gatifloxacin. 20 compounds were synthesized in this study. Among them 2,3 and 4 were known compounds, others new compounds, whose structure had been determined by NMR and MS or HRMS. |
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| Keywords: | Fluoroquinolone Synthesis Antibacterial activity |
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