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Ammonium and guanidine carbosilane dendrimers and dendrons as microbicides
European Polymer Journal ( IF 5.8 ) Pub Date : 2018-04-01 , DOI: 10.1016/j.eurpolymj.2018.02.025
Irene Heredero-Bermejo , José M. Hernández-Ros , Leticia Sánchez-García , Marek Maly , Cristina Verdú-Expósito , Juan Soliveri , F. Javier de la Mata , José L. Copa-Patiño , Jorge Pérez-Serrano , Javier Sánchez-Nieves , Rafael Gómez

Abstract Carbosilane dendrimers (generations 1–3) and dendrons (generations 2–3) functionalized with guanidine functions (GU) have been synthesized from corresponding ammonium (–NH3+) derivatives with good yield. These dendritic molecules were tested as microbicides against Escherichia coli (Gram-negative), Staphylococcus aureus (Gram-positive) and methicillin resistant S. aureus (MRSA) bacteria; and against Acanthomoeba polyphaga in both stages, trophozoites and cysts. The best results were obtained for lower generation dendrimers and dendrons, with no remarkable influence of the peripheral moieties against bacteria but with better amoebicide activity for –NH3+ systems. Moreover, the activity values of first generation dendrimers and second generation dendrons were below their cytotoxicity against eukaryote cells. Molecular dynamics study of interactions between selected dendrimers and anionic phospholipid bilayers indicates possible connections between the antibacterial activity and interaction modes.

中文翻译:

作为杀微生物剂的铵和胍碳硅烷树枝状聚合物和树枝状化合物

摘要 已从相应的铵 (–NH3+) 衍生物中以良好的收率合成了用胍官能团 (GU) 功能化的碳硅烷树枝状聚合物(第 1-3 代)和树枝状大分子(第 2-3 代)。这些树突状分子被测试为针对大肠杆菌(革兰氏阴性)、金黄色葡萄球菌(革兰氏阳性)和耐甲氧西林金黄色葡萄球菌 (MRSA) 细菌的杀微生物剂;并针对两个阶段的多食棘阿米巴,滋养体和包囊。低代树枝状大分子和树枝状分子获得了最好的结果,外围部分对细菌没有显着影响,但对 –NH3+ 系统具有更好的阿米巴杀虫活性。此外,第一代树枝状聚合物和第二代树枝状聚合物的活性值低于它们对真核细胞的细胞毒性。
更新日期:2018-04-01
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