These superior, highly potent N-Arylated NH125 analogues demonstrate broad-spectrum antibacterial activities against even drug-resistant strains and are promising agents for disinfectants and antiseptics that eradicate bacteria, biofilms and persister cells. Biofilms are pervasive, surface-attached colonies of bacteria or other microorganisms that form a protective extracellular matrix, making them difficult to kill. Biofilms with dormant persister cells are highly tolerant of antibiotics and biocides. Persister cells of methicillin-resistant Staphylococcus aureus (MRSA) play a major role in the 100,000 serious infections and 18,000 deaths yearly, with treatments resulting in $4 billion in costs in the United States alone. Researchers at the University of Florida have developed powerful N-arylated NH125 analogues that have proven to be potent and rapid in killing MRSA persister cells in stationary cultures when compared to a panel of membrane-targeting antimicrobial peptides, including quaternary ammonium cations.
N-arylated NH125 analogues act as potent antibacterial agents, biofilm eradicators, and MRSA persister cell killers
Researchers at the University of Florida have modified the arrangement of the anti-bacterial compound, NH125, into two distinct N-Arylated analogues that kill MRSA persister cells and other resistant bacteria. Similar to NH125, the analogues have a long aliphatic tail and an imidazole heterocycle that contains a charged nitrogen atom. This arrangement enables the chemical to rupture the bacterial membranes, killing them. Additionally, the NH125 structure has an N-arylated-2-methylimidazole heterocycle which is augmented in the analogues to contain an additional functional group. This allows the chemical agents to better target bacterial or fungal cells. When tested against MRSA, methicillin-resistant Staphylococcus epidermis (MRSE), and vancomycin-resistant Enterococcus faecium (VRE), the analogues outperformed all other membrane-targeting antibacterial agents.
