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 |
|---|---|
| pagine (da-a) | 6819-6825 |
| Numero di pagine | 7 |
| Rivista | BIOORGANIC & MEDICINAL CHEMISTRY |
| Volume | 22 |
| Stato di pubblicazione | Published - 2014 |
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All Science Journal Classification (ASJC) codes
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
Cita questo
Palumbo Piccionello, A., Pace, A., Guarcello, A., Lonati, E., Caltabiano, G., Guarcello, A., Pace, A., Bonaccorso, C., Berardozzi, R., Musumarra, G., Pescitelli, G., Pierro, P., Bulbarelli, A., Goracci, L., Fortuna, C. G., Di Bari, L., Cocuzza, C. E. A., Musumeci, R., Palumbo Piccionello, A., & Pierro, P. (2014). New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles. BIOORGANIC & MEDICINAL CHEMISTRY, 22, 6819-6825.