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

[Display omitted] 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 pho...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2020-09, Vol.30 (18), p.127389-127389, Article 127389
Hauptverfasser: Brunel, Frédéric, Lautard, Christelle, Garzino, Frédéric, Raimundo, Jean-Manuel, Bolla, Jean-Michel, Camplo, Michel
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Sprache:eng
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Zusammenfassung:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127389