Antimicrobial and Antibiofilm Activity of Disubstituted Bis‐benzimidazolium Salts,ChemMedChem

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Antimicrobial and Antibiofilm Activity of Disubstituted Bis‐benzimidazolium Salts
ChemMedChem ( IF 3.6 ) Pub Date : 2018-11-19 , DOI: 10.1002/cmdc.201800639
Jérémie Tessier ₁ , Margaux Lecluse ₁ , Julien Gravel ₁ , Andreea‐Ruxandra Schmitzer ₁

Affiliation

The increased prevalence of antibiotic‐resistant bacteria is a critical issue for human health. Developing new antibiotic agents is vital for fighting persistent infections and lowering mortality rates. In this study, we designed lutidine‐disubstituted bis‐benzimidazolium salts (lutidine‐bis‐benzimidazolium core with octyl, adamantyl, and cholesteryl lipophilic side chains), and tested their antimicrobial activity, their capacity to inhibit planktonic bacterial and fungal growth, and their ability to inhibit the formation of or disrupt mature methicillin‐resistant Staphylococcus aureus (MRSA) biofilms. The antibiofilm activity of these salts was analyzed in terms of their lipophilicity, capacity to induce transmembrane ion transport, perturbation of the cellular membrane, and mechanism of action in the phospholipid bilayer. The synthesized compounds were not active against MRSA biofilms, as the formation of transmembrane channels had no effect on the integrity of the extracellular polymeric substance matrix and only octyl and adamantyl derivatives possessed the capacity to inhibit biofilm formation. The synthesized derivatives could be used as lead candidates for the development of anti‐MRSA agents.

中文翻译：

双取代双苯并咪唑鎓盐的抗菌和生物膜活性

抗生素耐药细菌的流行是人类健康的关键问题。开发新的抗生素对抵抗持续感染和降低死亡率至关重要。在这项研究中，我们设计了二甲基联苯二甲基双联苯并咪唑鎓盐（具有辛基，金刚烷基和胆固醇基亲脂性侧链的联苯二甲基双联苯并咪唑鎓盐），并测试了它们的抗菌活性，抑制浮游细菌和真菌生长的能力及其抑制耐甲氧西林金黄色葡萄球菌形成或破坏其能力（MRSA）生物膜。根据它们的亲脂性，诱导跨膜离子转运的能力，细胞膜的扰动以及磷脂双层中的作用机理，分析了这些盐的抗生物膜活性。合成的化合物对MRSA生物膜没有活性，因为跨膜通道的形成对细胞外聚合物基质的完整性没有影响，只有辛基和金刚烷基衍生物才具有抑制生物膜形成的能力。合成的衍生物可用作开发抗MRSA药物的主要候选药物。

更新日期：2018-11-19

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