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

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

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Abstract

© 2014 Elsevier Ltd. All rights reserved. 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.
Original languageEnglish
Pages (from-to)6814-6825
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number24
DOIs
Publication statusPublished - 15 Dec 2014

Keywords

  • Antibiotics
  • Drug design
  • Enantiomers
  • Linezolid
  • Multidrug-resistant bacteria

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