New potent antibacterials against Gram-positive multiresistantpathogens: Effects of side chain modification and chirality inlinezolid-like 1,2,4-oxadiazoles

Antonio Palumbo Piccionello, Andrea Pace, Annalisa Guarcello, Elena Lonati, Gianluigi Caltabiano, Annalisa Guarcello, Andrea Pace, Carmela Bonaccorso, Roberto Berardozzi, Giuseppe Musumarra, Gennaro Pescitelli, Paola Pierro, Alessandra Bulbarelli, Laura Goracci, Cosimo G. Fortuna, Lorenzo Di Bari, Clementina E.A. Cocuzza, Rosario Musumeci, Antonio Palumbo Piccionello, Paola Pierro

Research output: Contribution to journalArticle

9 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)6819-6825
Number of pages7
JournalBIOORGANIC & MEDICINAL CHEMISTRY
Volume22
Publication statusPublished - 2014

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    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.