Abstract The synthesis and antibacterial activity of 3-(4-([1, 2, 4] triazolo [4, 3-a] pyrimidin-3- yl) phenyl) oxazolidin-2-ones is reported. Thiocarbonyl derivatives were found to be potent inhibitors of Gram-positive pathogens and compound 4l was two to fourfold more potent than Linezolid.