%0 Journal Article 
%A Fuentes Paniagua, María Elena
%A Sánchez-Nieves Fernández, Javier
%A Hernández Ros, José Manuel
%A Fernández Ezequiel, Alba
%A Soliveri De Carranza, Juan
%A Copa Patiño, José Luis
%A Gómez Ramírez, Rafael
%A Mata de la Mata, Francisco Javier de la
%T Structure-activity relationship study of cationic carbosilane dendritic systems as antibacterial agents
%D 2016
%@ 2046-2069
%U http://hdl.handle.net/10017/34040
%X This work focuses on the antibacterial activity against Gram-positive Staphylococcus aureus and Gramnegative Escherichia coli and the hemolytic properties of two types of ammonium cationic carbosilane systems: dendrimers and dendrons. The effects of: i) the generation, ii) the type of peripheral groups near
the cationic charges (a SiMe2 moiety or a S atom depending on the synthetic procedure, hydrosilylation or
thiol-ene addition, respectively), iii) the core of dendrimers (polyphenoxo vs. Si atom) and iv) the focal
point of dendrons (-N3, -NH2, -OH) have been assessed. The structure-activity relationship analysis
indicates the importance of an adequate balance between the hydrophilic and lipophilic fragments of these
molecules to reach the best antibacterial activity. Regarding hemolysis, lowest toxicity values were
registered for dendritic systems with a sulfur atom close to the surface and, in the particular case of
dendrons, for those with a hydroxyl focal point. One dendrimer and one dendron, both bearing a sulfur
atom close to the surface, scored best in the activity-toxicity relationship analysis and were chosen for
resistance assays. No changes in the inhibitory and bactericidal capacity in the case of the dendron and only
a slight increase of these values for the dendrimer were observed after 15 subculture cycles. Furthermore,
these two compounds stayed active towards different strains of resistant bacteria and avoid formation of
biofilm at concentrations over the minimum inhibitory concentration (MIC).
%K Dendritic
%K Cationic
%K Antibacterial
%K Resistance assay
%K Biofilm
%K Chemistry
%K Química
%~ Biblioteca Universidad de Alcala