Synthesis of triazole-functionalized 2-DOS analogues and their evaluation as A-site binders
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- 作者：Panoula Anastasopoulou ; Georgia Kythreoti ; Tilemachos Cosmidis ; Constantina Pyrkotis ; Victoria R. Nahmias ; Dionisios Vourloumis
- 关键词：Aminoglycosides ; Ribosomal A-site ; RNA recognition ; 2-Deoxystreptamine ; Orthogonal protection strategy
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：15 February, 2014
- 年：2014
- 卷：24
- 期：4
- 页码：1122-1126
- 全文大小：661 K
文摘
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.