Amidine-Based Cationic Conjugated Oligoelectrolytes with Antimicrobial Activity against Pseudomonas aeruginosa Biofilms.

Journal of medicinal chemistry(2023)

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摘要
is an opportunistic Gram-negative bacterium that can cause high-morbidity infections. Due to its robust, flexible genome and ability to form biofilms, it can evade and rapidly develop resistance to antibiotics. Cationic conjugated oligoelectrolytes (COEs) have emerged as a promising class of antimicrobials. Herein, we report a series of amidine-containing COEs with high selectivity for bacteria. From this series, we identified as the most active compound against (minimum inhibitory concentration (MIC) = 2 μg/mL) with low cytotoxicity (IC (HepG2) = 1024 μg/mL). The activity of was not affected by known drug-resistant phenotypes of 100 diverse isolates. Moreover, is bactericidal with a low propensity for to develop resistance. Furthermore, is also able to inhibit biofilm formation at subinhibitory concentrations and kills in established biofilms. The efficacy of was demonstrated in biofilm-associated murine wound infection models.
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关键词
cationic conjugated oligoelectrolytes,antimicrobial activity,amidine-based
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