Phosphonium-ammonium-based di-cationic ionic liquids as antibacterial over the ESKAPE group

被引:24
作者
Brunel, Frederic [1 ]
Lautard, Christelle [2 ]
Garzino, Frederic [1 ]
Raimundo, Jean-Manuel [1 ]
Bolla, Jean-Michel [2 ]
Camplo, Michel [1 ]
机构
[1] Aix Marseille Univ, CNRS, CINaM UMR 7325, Campus Luminy,Case 913, F-13288 Marseille 09, France
[2] Aix Marseille Univ, MCT, SSA, INSERM, 27 Blvd Jean Moulin, F-13385 Marseille 05, France
关键词
Antimicrobial; Phosphonium and ammonium derivatives; Ionic liquids; PYRIDINIUM SALTS; IMIDAZOLIUM; PATHOGENS;
D O I
10.1016/j.bmcl.2020.127389
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Emergence of antibioresistance is currently a major threat of public health worldwide. Hence there is an urge need of finding new antibacterial material. Herein, we report a simple and eco-friendly method to synthesize homo and heterodicationic ionic liquids based on quaternary phosphonium and ammonium salt. In order to investigate the structure activity relationship (SAR) we measured the MICs of a series of 16 derivatives with structural variations (nature of cations and counter-ions, size of linker and alkyl side chains as well as structural symmetry) over a range of Gram-positive and Gram-negative bacterial strains from the ESKAPE group. Some of the tested structures exhibit high antimicrobial activities (MIC = 0.5 mg/L) and are active over a wide range of bacteria from Gram-positive to Gram-negative. Overall, these results reveal the strong potential of di-cationic derivatives as antibacterial agents and the determination of activities from structural features gives decisive information for future synthesis of such di-cationic structures for biocidal purpose.
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页数:4
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