| 羟基修饰与药物抗菌活性研究进展 |
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| 引用本文： | 何小燕,李逐波.羟基修饰与药物抗菌活性研究进展[J].中国兽药杂志,2006,40(6):45-48. |
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| 作者姓名： | 何小燕 李逐波 |
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| 作者单位： | 1. 西南大学动物科技学院,重庆北碚,400716
2. 西南大学药用资源化学研究所,重庆北碚,400716 |
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| 摘 要： | 修饰羟基可提高大多数抗菌药物的药效,研究中一般对羟基进行以下4种修饰：酰化为酰胺或酯类;烷化或烷氧化;用卤素取代;直接将羟基去除.经这些修饰后,可起到增强抗菌活性、对抗耐药性、方便制剂的作用,但羟基的修饰并非对所有的抗菌药物都是有利的,所以在修饰羟基时应视具体情况而定.
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| 关 键 词： | 羟基修饰 抗菌药物 活性 |
| 文章编号： | 1002-1280（2006）06-0045-04 |
| 收稿时间： | 2005-10-24 |
| 修稿时间： | 2005年10月24 |
Progress in Hydroxyl Structure-activity Relationship Study of Antibiotics |
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| HE Xiao-yan,LI Zhu-bo.Progress in Hydroxyl Structure-activity Relationship Study of Antibiotics[J].Chinese Journal of Veterinary Drug,2006,40(6):45-48. |
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| Authors: | HE Xiao-yan LI Zhu-bo |
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| Institution: | 1. Institute of Animal Science, Southwest University, Beipei, Chongqing 400716 ;2. Medical Resource Chemistry, Southwest University, Beipei, Chongqing 400716 ; China |
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| Abstract: | Modify antibiotics structure in terms of increased therapeutic effectiveness, reduced activity on multi drug resistance or both. Previous hydroxyl structure-activity studies had shown that modifications of the hydroxyl structure can result not only in active agents, but more importantly, analogues with reduced activity on drug resistance. The fact that hydroxyl derivatives showed higher potency than pre-antibiotics, prompted us to explore novel analogues with altered substitution patterns on the hydroxyl. In this paper it is described that hydroxyl was either removed or replaced with acyl or alkyl or halobiont groups. |
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| Keywords: | hydroxyl antibiotics modify |
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