Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains
Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains
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针对耐药菌株的强效氨基糖苷类抗生素的合理设计与合成
DOI：
10.1016/j.bmc.2010.11.065
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发表时间：
2011-01-01
影响因子：
3.5
通讯作者：
Ye, Xin-Shan
中科院分区：
文献类型：
--
作者：
Yan, Ri-Bai;Yuan, Min;Ye, Xin-Shan
根据生物大分子-氨基糖苷复合物的结构信息，合理设计并合成了一系列卡那霉素B类似物。本文提出了一种简便的构建卡那霉素衍生物的方法，即对卡那霉素第1环上的邻胺部分C4′位置进行修饰。大多数合成类似物对一些典型的耐药细菌表现出良好到优异的抗菌活性。结果表明，氨基糖苷类如卡那霉素的C4'-位置可能是获得新的耐酶修饰氨基糖苷类抗生素的理想修饰位点。(C) 2010 Elsevier Ltd.版权所有。
Based on the structural information of biomacromolecule-aminoglycoside complexes, a series of kanamycin B analogues were rationally designed and synthesized. A convenient approach to the construction of kanamycin derivatives, in which the C4'-position on ring I of neamine moiety was modified, was developed. Most synthetic analogues exhibited good to excellent antibiotic activity against some typical drug-resistant bacteria. The disclosed results suggested that the C4'-position of aminoglycosides such as kanamycin may be an ideal site for modification to gain new modifying enzyme-resistant aminoglycoside antibiotics. (C) 2010 Elsevier Ltd. All rights reserved.