New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics

Substitution of phenyl oxazolidinones with carbon-linked azoles resulted in the discovery of a new class of potent oxazolidinones that have excellent Gram-positive activity. In addition, replacement of the C-5 acetamide side chains with a 4-methyl triazole diminished monoamine oxidase activity. The synthesis and biological evaluation of these compounds are reported.

Graphical abstractThe synthesis, and the in vitro and in vivo evaluation of a new series of potent oxazolidinones are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide