An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria

Amit Kaushik, Abigail M. Heuer, Drew T. Bell, Jeffrey C. Culhane, David C. Ebner, Nicole Parrish, J. Thomas Ippoliti, Gyanu Lamichhane

Research output: Contribution to journalArticlepeer-review

Abstract

Innovation of new antibacterials that are effective against strains that have developed resistance to existing drugs would strengthen our ability to treat and subsequently control spread of pathogenic bacteria. Increasing incidence of infections with drug resistant bacteria has become a common occurrence in recent times. We have developed an evolved oxazolidinone, T145, which inhibits growth of Enterococcus faecalis, Staphylococcus aureus and Mycobacterium tuberculosis (Mtb) with sub μg/ml potencies that are potentially therapeutically valuable. The oxazolidinone is bactericidal against Mtb but bacteriostatic against E. faecalis and S. aureus. In addition to therapeutically valuable potency and bactericidal activity against Mtb, T145 minimizes selection of spontaneous resistant mutants, a trait that prolongs longevity of a drug in clinical use.

Original languageEnglish (US)
Pages (from-to)3572-3576
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number15
DOIs
StatePublished - 2016

Keywords

  • Antimicrobials
  • E. faecalis
  • Mycobacterium tuberculosis
  • Oxazolidinone
  • Staphylococcus aureus

ASJC Scopus subject areas

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

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