Abstract: Aim To study the structure-activity relationship of antibacterial oxazolidinone derivatives. Methods Seven (S)-5-(heterocycle methylene)-3-(3-fluoro-4-morpholin-4-yl-phenyl)-oxazolidin-2-ones were synthesized by the substitution of (S)-[3-(3-fluoro-4-morpholin-4-yl-phenyl)-oxazolidin-2-one-5-yl]-methanol mesylate with some secondary amines and the structures of the product were confirmed by ¹H NMR and elemental analyses or MS. Results None of the seven compounds showed potent activity against the tested 20 strains of bacteria in vitro. Conclusion The replacement of 5-acetylaminometyl of Linezolid by 5-(heterocycle methylene) lost the antibacterial activity.

Key words: oxazolidinone, oxazolidinone, antibacterial activity, antibacterial activity, synthesis, synthesis