Synthesis of triazole-functionalized 2-DOS analogues and their evaluation as A-site binders
Synthesis of triazole-functionalized 2-DOS analogues and their evaluation as A-site binders
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DOI：
10.1016/j.bmcl.2013.12.125
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发表时间：
2014-02-15
影响因子：
2.7
通讯作者：
Vourloumis, Dionisios
中科院分区：
文献类型：
--
作者：
Anastasopoulou, Panoula;Kythreoti, Georgia;Vourloumis, Dionisios
氨基糖苷类抗生素是研究RNA生物学功能的重要工具。应用于2-脱氧链霉胺（2-DOS）的正交保护策略揭示了一系列使其区域选择性官能化的关键中间体。我们的方法允许建设选定的代表性的三唑类化合物与不同的分子框架的生物学评价，其结合和抗菌效力。(C)2014爱思唯尔有限公司版权所有。
Aminoglycoside-antibiotics represent important tools for studying the biological functions of RNA. An orthogonal protection strategy applied on 2-deoxystreptamine (2-DOS) revealed a series of key intermediates that enable its regioselective functionalization. Our approach allowed the construction of selected representatives of triazole-containing analogues with diverse molecular frameworks for biological evaluation regarding their binding and antibacterial potencies. (C) 2014 Elsevier Ltd. All rights reserved.