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 M Parrish, J. Thomas Ippoliti, Gyanu Lamichhane

Research output: Contribution to journalArticle

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)
JournalBioorganic and Medicinal Chemistry Letters
DOIs
StateAccepted/In press - Apr 19 2016

Fingerprint

Oxazolidinones
Gram-Positive Bacteria
Mycobacterium tuberculosis
Bacteria
Enterococcus faecalis
Staphylococcus aureus
Pharmaceutical Preparations
Innovation
Incidence
Growth
Infection

Keywords

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

ASJC Scopus subject areas

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

Cite this

An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria. / Kaushik, Amit; Heuer, Abigail M.; Bell, Drew T.; Culhane, Jeffrey C.; Ebner, David C.; Parrish, Nicole M; Ippoliti, J. Thomas; Lamichhane, Gyanu.

In: Bioorganic and Medicinal Chemistry Letters, 19.04.2016.

Research output: Contribution to journalArticle

Kaushik, Amit ; Heuer, Abigail M. ; Bell, Drew T. ; Culhane, Jeffrey C. ; Ebner, David C. ; Parrish, Nicole M ; Ippoliti, J. Thomas ; Lamichhane, Gyanu. / An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria. In: Bioorganic and Medicinal Chemistry Letters. 2016.
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