Structure–activity studies of RNA-binding oxazolidinone derivatives

Abstract: 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. [Copyright &y& Elsevier]