Abstract
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.
Lingua originale | English |
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pagine (da-a) | 6819-6825 |
Numero di pagine | 7 |
Rivista | BIOORGANIC & MEDICINAL CHEMISTRY |
Volume | 22 |
Stato di pubblicazione | Published - 2014 |
All Science Journal Classification (ASJC) codes
- ???subjectarea.asjc.1300.1303???
- ???subjectarea.asjc.1300.1313???
- ???subjectarea.asjc.1300.1312???
- ???subjectarea.asjc.3000.3003???
- ???subjectarea.asjc.3000.3002???
- ???subjectarea.asjc.1300.1308???
- ???subjectarea.asjc.1600.1605???