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

Keith D. Green, Allan H. Pang, Nishad Thamban Chandrika, Atefeh Garzan, Anthony D. Baughn, Oleg V. Tsodikov, Sylvie Garneau-Tsodikova

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)757-767
Number of pages11
JournalACS Infectious Diseases
Volume8
Issue number4
DOIs
StatePublished - Apr 8 2022

Bibliographical note

Publisher Copyright:
© 2022 American Chemical Society. All rights reserved.

Keywords

  • MRSA
  • antibiotic
  • biofilm
  • drug discovery
  • structure-activity relationship

ASJC Scopus subject areas

  • Infectious Diseases

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