期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 13, 期 41, 页码 10290-10294出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ob01883h
关键词
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资金
- Emerging Pathogens Institute
- College of Pharmacy at the University of Florida
Small molecules capable of eradicating non-replicating bacterial biofilms are of great importance to human health as conventional antibiotics are ineffective against these surface-attached bacterial communities. Here, we report the discovery of several halogenated quinolines (HQs) identified through a reductive amination reaction that demonstrated potent eradication of MRSA (HQ-6; MBEC = 125 mu M), MRSE (HQ-3; MBEC = 3.0 mu M) and VRE (HQ-4, HQ-5 and HQ-6; MBEC = 1.0 mu M) biofilms. HQs were evaluated using the Calgary Biofilm Device (CBD) and demonstrated near equipotent killing activities against planktonic and biofilm cells based on MBC and MBEC values. When tested against red blood cells, these HQ analogues demonstrated low haemolytic activity (3 to 21% at 200 mu M) thus we conclude that these HQ analogues do not operate primarily through the destruction of bacterial membranes, typical of other biofilm-eradicating agents (i.e., antimicrobial peptides). HQ antibacterial agents are potent biofilm-eradicating compounds and could lead to useful treatments for biofilm-associated bacterial infections.
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