Jump to main content
Jump to site search

Issue 26, 2017
Previous Article Next Article

Antimicrobial peptide-inspired NH125 analogues: bacterial and fungal biofilm-eradicating agents and rapid killers of MRSA persisters

Author affiliations

Abstract

During microbial infection, antimicrobial peptides are utilized by the immune response to rapidly eradicate microbial pathogens through the destruction of cellular membranes. Inspired by antimicrobial peptides, quaternary ammonium cationic (QAC) compounds have emerged as agents capable of destroying bacterial membranes leading to rapid bacterial death, including the eradication of persistent, surface-attached bacterial biofilms. NH125, an imidazolium cation with a sixteen membered fatty tail, was recently reported to eradicate persister cells and was our starting point for the development of novel antimicrobial agents. Here, we describe the design, chemical synthesis and biological investigations of a collection of 30 diverse NH125 analogues which provided critical insights into structural features that are important for antimicrobial activities in this class. From these studies, multiple NH125 analogues were identified to possess potent antibacterial and antifungal activities, eradicate both bacterial and fungal biofilms and rapidly eradicate MRSA persister cells in stationary phase. NH125 analogues also demonstrated more rapid persister cell killing activities against MRSA when tested alongside a panel of diverse membrane-active agents, including BAC-16 and daptomycin. NH125 analogues could have a significant impact on persister- and biofilm-related problems in numerous biomedical applications.

Graphical abstract: Antimicrobial peptide-inspired NH125 analogues: bacterial and fungal biofilm-eradicating agents and rapid killers of MRSA persisters

Back to tab navigation

Supplementary files

Publication details

The article was received on 28 Apr 2017, accepted on 17 May 2017 and first published on 17 May 2017


Article type: Paper
DOI: 10.1039/C7OB01028A
Citation: Org. Biomol. Chem., 2017,15, 5503-5512
  •   Request permissions

    Antimicrobial peptide-inspired NH125 analogues: bacterial and fungal biofilm-eradicating agents and rapid killers of MRSA persisters

    A. Basak, Y. Abouelhassan, R. Zuo, H. Yousaf, Y. Ding and R. W. Huigens, Org. Biomol. Chem., 2017, 15, 5503
    DOI: 10.1039/C7OB01028A

Search articles by author

Spotlight

Advertisements