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.

Fortuna, C., Berardozzi, R., Bonaccorso, C., Caltabiano, G., Di Bari, L., Goracci, L., et al. (2014). New potent antibacterials against Gram-positive multiresistant pathogens: Effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles. BIOORGANIC & MEDICINAL CHEMISTRY, 22(24), 6814-6825 [10.1016/j.bmc.2014.10.037].

New potent antibacterials against Gram-positive multiresistant pathogens: Effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles

LONATI, ELENA RITA;BULBARELLI, ALESSANDRA;COCUZZA, CLEMENTINA ELVEZIA;MUSUMECI, ROSARIO
Ultimo
2014

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.
Articolo in rivista - Articolo scientifico
Scientifica
Drug design; Linezolid; Antibiotics; Multidrug-resistant bacteria; Enantiomers
English
Fortuna, C., Berardozzi, R., Bonaccorso, C., Caltabiano, G., Di Bari, L., Goracci, L., et al. (2014). New potent antibacterials against Gram-positive multiresistant pathogens: Effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles. BIOORGANIC & MEDICINAL CHEMISTRY, 22(24), 6814-6825 [10.1016/j.bmc.2014.10.037].
Fortuna, C; 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, C; Musumarra, G; Musumeci, R
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10281/55571
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