New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles

The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studiedto design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adoptedstrategy involved a molecular modelling approach, the synthesis and biological evaluation of newdesigned compounds, enantiomers separation and absolute configuration assignment. Experimentaldetermination of the antibacterial activity of the designed (S)-1-((3-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea and (S)-1-((3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea against multidrug resistantlinezolid bacterial strains was higher than that of linezolid.