Structure–activity studies of RNA-binding oxazolidinone derivatives

The structure–activity relationship of a series of oxazolidinones binding to T-box riboswitch antiterminator RNA has been investigated. Oxazolidinones differentially substituted at C-5 were prepared and the ligand-induced fluorescence resonance energy transfer (FRET) changes in FRET-labeled antiterminator model RNA were assayed. Both qualitative and quantitative analysis of the structure–activity relationship indicate that hydrogen bonding and hydrophobic properties play a significant role in ligand binding.

Graphical abstractStructure–activity studies of the acyl group of a set of oxazolidinones binding to T-box antiterminator RNA have been explored.Figure optionsDownload full-size imageDownload as PowerPoint slide