2. Academic Validation
  3. An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria

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

  • Bioorg Med Chem Lett. 2016 Aug 1;26(15):3572-6. doi: 10.1016/j.bmcl.2016.06.019.
Amit Kaushik 1,  Abigail M Heuer 2,  Drew T Bell 1,  Jeffrey C Culhane 2,  David C Ebner 2,  Nicole Parrish 3,  J Thomas Ippoliti 4,  Gyanu Lamichhane 5
Affiliations

Affiliations

  • 1 Taskforce to Study Resistance Emergence & Antimicrobial Development Technology and Center for Tuberculosis Research, Department of Medicine, Johns Hopkins University, 1550 Orleans St, Baltimore, MD 21287, United States.
  • 2 Department of Chemistry, University of St. Thomas, St. Paul, MN 55105, United States.
  • 3 Department of Pathology, Johns Hopkins University, Baltimore, MD 21205, United States.
  • 4 Department of Chemistry, University of St. Thomas, St. Paul, MN 55105, United States. Electronic address: jtippoliti@stthomas.edu.
  • 5 Taskforce to Study Resistance Emergence & Antimicrobial Development Technology and Center for Tuberculosis Research, Department of Medicine, Johns Hopkins University, 1550 Orleans St, Baltimore, MD 21287, United States. Electronic address: lamichhane@jhu.edu.
PMID: 27329794 DOI: 10.1016/j.bmcl.2016.06.019
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.

Keywords

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

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-113687
    Antibacterial Agent