抗生素结构修饰的进展
抗生素；,结构修饰,,抗生素；,结构修饰,1扩展抗菌谱的修饰,2增强抗菌活性的修饰,3克服耐药性的修饰,4改善药物动力学性能的修饰,5降低毒副反应的修饰,6适应制剂需要的修饰,7小结,参考文献
摘要： 天然抗生素结构的适当修饰可改善其性能，是探索开发新药的有效途径之一。本文综述抗生素结构修饰研究的现状与进展，列举了在扩展抗菌谱、增强抗菌活性、克服耐药性、改善药物动力学性能、降低毒副反应以及适应制剂需要等方面的成功修饰实例。不是所有抗生素经过修饰都能如愿地得到良好的修饰物，但在新抗生素筛选困难重重的今天，对获得的天然物进行适当的结构修饰是十分必要的。关键词： 抗生素； 结构修饰
Advances in structural modification of antibiotics
Zhang Zhiping
(Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences,Peking Union Medical College, Beijing 100050)
ABSTRACT Ingenious modification of structure of natural antibiotics could improve their properties, which is one of ways to search for new drugs. In this paper some successful examples of structural modifications in expansion of antibacterial spectrum, increase of antibacterial activities, relief of resistance, improvement of pharmacokinetic properties, alleviation of toxicity and requirement for preparation were summarized. Although wishful products could not be obtained from any antibiotic, which has been modified. In these days of difficulty to search for new antibiotics, the modification of structure of natural antibiotics is necessary.
KEY WORDS Antibiotics; Structural modification ......
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