Synthesis of triazole-functionalized 2-DOS analogues and their evaluation as A-site binders

Panoula Anastasopoulou, Georgia Kythreoti, Tilemachos Cosmidis, Constantina Pyrkotis, Victoria R. Nahmias, Dionisios Vourloumis

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1122-1126
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number4
DOIs
Publication statusPublished - 15 Feb 2014

Keywords

  • 2-Deoxystreptamine
  • Aminoglycosides
  • Orthogonal protection strategy
  • Ribosomal A-site
  • RNA recognition

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