Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent

Novel oxazolidinone antibacterials containing N-hydroxyacetamidine moiety are synthesized with the diversity at C-5 terminus. These compounds have been evaluated against a panel of clinically relevant Gram-positive and Gram-negative pathogens. Most of the analogs in this series displayed activity superior to Linezolid and in vivo efficacies of selected oxazolidinones are also disclosed herein.

Graphical abstractThe synthesis of oxazolidinones possessing N-hydroxyacetamidine group on piperazine scaffold and their in vitro antibacterial activity profile are disclosed herein.Figure optionsDownload full-size imageDownload as PowerPoint slide