Discovery and Optimization of 6-(1-Substituted pyrrole-2-yl)- s -triazine Containing Compounds as Antibacterial Agents.

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  • Additional Information
    • Source:
      Publisher: ACS Publications Country of Publication: United States NLM ID: 101654580 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2373-8227 (Electronic) Linking ISSN: 23738227 NLM ISO Abbreviation: ACS Infect Dis Subsets: MEDLINE
    • Publication Information:
      Original Publication: Washington, DC : ACS Publications, [2015]-
    • Subject Terms:
    • Abstract:
      Antimicrobial drug resistance is a major health issue plaguing healthcare worldwide and leading to hundreds of thousands of deaths globally each year. Tackling this problem requires discovery and development of new antibacterial agents. In this study, we discovered novel 6-(1-substituted pyrrole-2-yl)- s -triazine containing compounds that potently inhibited the growth of Staphylococcus aureus regardless of its methicillin-resistant status, displaying minimum inhibitory concentration (MIC) values as low as 1 μM. The presence of a single imidazole substituent was critical to the antibacterial activity of these compounds. Some of the compounds also inhibited several nontubercular mycobacteria. We have shown that these molecules are potent bacteriostatic agents and that they are nontoxic to mammalian cells at relevant concentrations. Further development of these compounds as novel antimicrobial agents will be aimed at expanding our armamentarium of antibiotics.
    • Grant Information:
      R01 AI100560 United States AI NIAID NIH HHS
    • Contributed Indexing:
      Keywords: MRSA; antibiotic; biofilm; drug discovery; structure−activity relationship
    • Accession Number:
      0 (Anti-Bacterial Agents)
      0 (Pyrroles)
      0 (Triazines)
    • Publication Date:
      Date Created: 20220303 Date Completed: 20220411 Latest Revision: 20220606
    • Publication Date:
      20240105
    • Accession Number:
      10.1021/acsinfecdis.1c00450
    • Accession Number:
      35239306