Halogenation of Biotin Protein Ligase Inhibitors Improves Whole Cell Activity against Staphylococcus aureus

Ashleigh S. Paparella, Kwang Jun Lee, Andrew J. Hayes, Jiage Feng, Zikai Feng, Danielle Cini, Sonali Deshmukh, Grant W. Booker, Matthew C.J. Wilce, Steven W. Polyak, Andrew D. Abell

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

We report the synthesis and evaluation of 5-halogenated-1,2,3-Triazoles as inhibitors of biotin protein ligase from Staphylococcus aureus. The halogenated compounds exhibit significantly improved antibacterial activity over their nonhalogenated counterparts. Importantly, the 5-fluoro-1,2,3-Triazole compound 4c displays antibacterial activity against S. aureus ATCC49775 with a minimum inhibitory concentration (MIC) of 8 μg/mL.

Original languageEnglish (US)
Pages (from-to)175-184
Number of pages10
JournalACS Infectious Diseases
Volume4
Issue number2
DOIs
StatePublished - Feb 9 2018

Keywords

  • antibiotic
  • biotin protein ligase
  • enzyme inhibitor
  • Staphylococcus aureus

ASJC Scopus subject areas

  • Infectious Diseases

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