Identification of a Novel Protein Synthesis Inhibitor Active against Gram-Positive Bacteria

Nora R. Eibergen, Isak Im, Nisha Y. Patel, Paul J. Hergenrother

Research output: Contribution to journalArticlepeer-review


In an effort to identify novel antibacterial chemotypes, we performed a whole-cell screen for inhibitors of Staphylococcus aureus growth and pursued those compounds with previously uncharacterized antibacterial activity. This process resulted in the identification of a benzothiazolium salt, ABTZ-1, that displayed potent antibacterial activity against Gram-positive pathogens. Several clinically desirable qualities were demonstrated for ABTZ-1 including potent activity against multidrug-resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant enterococci (VRE), retention of this activity in human serum, and low hemolytic activity. The antibacterial activity of ABTZ-1 was attributed to its inhibition of bacterial translation, as this compound prevented the incorporation of [ 35S]methionine into S. aureus proteins, and ABTZ-1-resistant strains were cross-resistant to known inhibitors of bacterial translation. ABTZ-1 represents a promising new class of antibacterial agents.

Original languageEnglish (US)
Pages (from-to)574-583
Number of pages10
Issue number4
StatePublished - Mar 2012


  • Antibacterials
  • Antibiotics
  • Benzothiazoles
  • MRSA
  • Staphylococcus aureus
  • Translation

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry


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