Novel promising linezolid analogues: Rational design, synthesis and biological evaluation

•5-Substituted oxazolidinones linezolid analogues were synthesized.•Docking studies of linezolid (thio)urea derivatives were performed.•Compound 10f demonstrated an activity comparable to that of linezolid.

A new series of 5-substituted oxazolidinones derived from linezolid, having urea and thiourea moieties at the C-5 side chain of the oxazolidinone ring, were prepared and their in vitro antibacterial activity was evaluated. The compound 10f demonstrated high antimicrobial activity, comparable to that of linezolid against Staphylococcus aureus.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide