New potent antibacterials against Gram-positive multiresistant pathogens: Effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles
- Authors: Fortuna, CG; Berardozzi, R; Bonaccorso, C; Caltabiano, G; Di Bari, L; Goracci, L; Guarcello, A; Pace, A; Palumbo Piccionello, A; Pescitelli, G; Pierro, P; Lonati, E; Bulbarelli, A; Cocuzza, CEA; Musumarra, G; Musumeci, R
- Publication year: 2014
- Type: Articolo in rivista (Articolo in rivista)
- OA Link: http://hdl.handle.net/10447/103056
Abstract
The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compounds, enantiomers separation and absolute configuration assignment. Experimental determination 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 resistant linezolid bacterial strains was higher than that of linezolid.