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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.

SUBMITTER: Maciagiewicz I 

PROVIDER: S-EPMC3466080 | biostudies-literature | 2011 Aug

REPOSITORIES: biostudies-literature

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Structure-activity studies of RNA-binding oxazolidinone derivatives.

Maciagiewicz Iwona I   Zhou Shu S   Bergmeier Stephen C SC   Hines Jennifer V JV  

Bioorganic & medicinal chemistry letters 20110615 15


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 li  ...[more]

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