Department of Chemistry, The University of Western Ontario, 1151 Richmond St., London, ON, N6A 3K7, Canada.
Department of Chemical and Biochemical Engineering, 1151 Richmond St., London, ON, N6A 3K7, Canada.
Angew Chem Int Ed Engl. 2018 Sep 24;57(39):12707-12710. doi: 10.1002/anie.201806412. Epub 2018 Aug 30.
There is currently an urgent need for the development of new antibacterial agents to combat the spread of antibiotic-resistant bacteria. We explored the synthesis and antibacterial activities of novel, sugar-functionalized phosphonium polymers. While these compounds exhibited antibacterial activity, we unexpectedly found that the control polymer poly(tris(hydroxypropyl)vinylbenzylphosphonium chloride) showed very high activity against both Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus and very low haemolytic activity against red blood cells. These results challenge the conventional wisdom in the field that lipophilic alkyl substituents are required for high antibacterial activity and opens prospects for new classes of antibacterial polymers.
目前迫切需要开发新的抗菌剂来对抗抗生素耐药菌的传播。我们探索了新型糖功能化膦聚合物的合成和抗菌活性。虽然这些化合物表现出抗菌活性，但我们出人意料地发现，对照聚合物聚（三羟丙基乙烯基苯膦氯）对革兰氏阴性大肠杆菌和革兰氏阳性金黄色葡萄球菌均显示出非常高的活性，对红细胞的溶血活性非常低。这些结果挑战了该领域的传统观点，即亲脂性烷基取代基是高抗菌活性所必需的，并为新型抗菌聚合物开辟了前景。
