Nowadays, the emergence of superbugs is one of the most serious public health problems. Strains of Staphylococcus aureus and Klebsiella pneumoniae, resistant to many antimicrobials available in clinical practice, have become increasingly common. The development of new drugs for the treatment of infections caused by these pathogens is necessary and urgent. A series of 11 analogs of marine 3-alkylpyridine alkaloids was evaluated in vitro for its antibacterial potential. Compound 6, a synthetic analog of viscosaline, exhibited significant activity against S. aureus, including an MRSA strain (MIC = 2 µg/mL). Additionally, it exhibited a 25% reduction in mature biofilm and a good selectivity index (SI > 16). None of the compounds exhibited activity against K. pneumoniae, but analog 6 was able to act in planktonic cells in the presence of polymyxin B at sub-inhibitory concentration. Compound 6 has promising anti-staphylococcal activity and future assays are encouraged to investigate their therapeutic potential.

中文翻译：

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3-烷基吡啶海洋生物碱合成类似物的抗菌和生物膜活性

如今，超级细菌的出现是最严重的公共卫生问题之一。对临床实践中可用的许多抗菌素具有耐药性的金黄色葡萄球菌和肺炎克雷伯菌菌株已变得越来越普遍。开发用于治疗由这些病原体引起的感染的新药物是必要和紧迫的。在体外评估了海洋3-烷基吡啶生物碱的一系列11种类似物的抗菌潜力。化合物6（粘胶碱的合成类似物）对金黄色葡萄球菌具有显着活性，包括MRSA菌株（MIC = 2 µg / mL）。此外，它还显示出成熟生物膜减少了25％，选择性指数良好（SI> 16）。这些化合物均未显示出抗肺炎克雷伯菌的活性，但类似物6能够在亚抑制浓度的多粘菌素B存在下在浮游细胞中起作用。化合物6具有令人信服的抗葡萄球菌活性，因此鼓励未来的分析方法研究其治疗潜力。