TY - JOUR
T1 - New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles
AU - Palumbo Piccionello, Antonio
AU - Guarcello, Annalisa
AU - Pace, Andrea
AU - Lonati, Elena
AU - Caltabiano, Gianluigi
AU - Guarcello, Annalisa
AU - Pace, Andrea
AU - Bonaccorso, Carmela
AU - Berardozzi, Roberto
AU - Musumarra, Giuseppe
AU - Pescitelli, Gennaro
AU - Pierro, Paola
AU - Bulbarelli, Alessandra
AU - Goracci, Laura
AU - Fortuna, Cosimo G.
AU - Di Bari, Lorenzo
AU - Cocuzza, Clementina E.A.
AU - Musumeci, Rosario
AU - Palumbo Piccionello, Antonio
AU - Pierro, Paola
PY - 2014
Y1 - 2014
N2 - 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.
AB - 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.
UR - http://hdl.handle.net/10447/103056
M3 - Article
VL - 22
SP - 6819
EP - 6825
JO - BIOORGANIC & MEDICINAL CHEMISTRY
JF - BIOORGANIC & MEDICINAL CHEMISTRY
SN - 0968-0896
ER -