| 选择性封闭卡那霉素A耐药酶羟基衍生物的合成 |
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| 引用本文： | 陈颖,孟祥豹,陈桂辉,潘攀,李中军. 选择性封闭卡那霉素A耐药酶羟基衍生物的合成[J]. 中国药学, 2008, 17(2): 138-143 |
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| 作者姓名： | 陈颖 孟祥豹 陈桂辉 潘攀 李中军 |
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| 作者单位： | 北京大学药学院天然药物及仿生药物国家重点实验室 化学生物学系,北京100083 |
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| 基金项目： | 国家重点基础研究发展计划(973计划) |
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| 摘 要： | 为寻找能抵抗耐药酶作用的氨基糖苷类抗生素，本文对卡那霉素A的3＇-OH，4＇-OH和2＂-OH位点进行了修饰。合成路线中的关键中间体为引入双苄叉保护基的卡那霉素A衍生物。目标羟基通过苄基化，甲基化和烯丙基化的方法进行修饰。最后通过多步反应脱保护，得到目标产物。活性结果显示，目标产物对敏感菌和耐药菌未显示出良好的抗菌活性。
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| 关 键 词： | 氨基糖苷 卡那霉素A衍生物 耐药酶 区域选择性 |
Synthesis of kanamycin A derivatives by regioselective masking drug resistant enzymes targeting hydroxyl groups |
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| Ying Chen,Xiang-Bao Meng,Gui-Hui Chen,Pan Pan,Zhong-Jun Li. Synthesis of kanamycin A derivatives by regioselective masking drug resistant enzymes targeting hydroxyl groups[J]. Journal of Chinese Pharmaceutical Sciences, 2008, 17(2): 138-143 |
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| Authors: | Ying Chen Xiang-Bao Meng Gui-Hui Chen Pan Pan Zhong-Jun Li |
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| Affiliation: | ( The State Key Laboratory of Natural and Biomimetic drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China ) |
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| Abstract: | The 3＇-OH, 4＇-OH and 2＂-OH of kanamycin A were modified in search of new aminoglycosides to overcome resistant enzymes, ANTs and APHs. The key intermediate was a dibenzylidene-protected derivative of kanamycin A. The aimed sites were masked by benzyl, methyl and allyl groups. Multi-step reactions gave the desired aminoglycoside derivatives but showed less antibiotic activity than kanamycin A. |
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| Keywords: | Aminoglycoisdes Kanamycin A derivatives Resistant enzyme Regioselectivity |
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