Ammonium and guanidine carbosilane dendrimers and dendrons as microbicides

作者：Heredero Bermejo Irene; Hernandez Ros Jose M; Sanchez Garcia Leticia; Maly Marek; Verdu Exposito Cristina; Soliveri Juan; Javier de la Mata F; Copa Patino Jose L; Perez Serrano Jorge; Sanchez Nieves Javier^*; Gomez Rafael^*

来源：European Polymer Journal, 2018, 101: 159-168.

DOI：10.1016/j.eurpolymj.2018.02.025

• Carbosilane dendrimers
• Ammonium
• Guanidine
• Antibacterial
• Amoebicide
• Molecular dynamics

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 (MESA) 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.

• 出版日期2018-4