RT info:eu-repo/semantics/article T1 Structure-activity relationship study of cationic carbosilane dendritic systems as antibacterial agents A1 Fuentes Paniagua, María Elena A1 Sánchez-Nieves Fernández, Javier A1 Hernández Ros, José Manuel A1 Fernández Ezequiel, Alba A1 Soliveri De Carranza, Juan A1 Copa Patiño, José Luis A1 Gómez Ramírez, Rafael A1 Mata de la Mata, Francisco Javier de la K1 Dendritic K1 Cationic K1 Antibacterial K1 Resistance assay K1 Biofilm K1 Chemistry K1 Química AB 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 nearthe cationic charges (a SiMe2 moiety or a S atom depending on the synthetic procedure, hydrosilylation orthiol-ene addition, respectively), iii) the core of dendrimers (polyphenoxo vs. Si atom) and iv) the focalpoint of dendrons (-N3, -NH2, -OH) have been assessed. The structure-activity relationship analysisindicates the importance of an adequate balance between the hydrophilic and lipophilic fragments of thesemolecules to reach the best antibacterial activity. Regarding hemolysis, lowest toxicity values wereregistered for dendritic systems with a sulfur atom close to the surface and, in the particular case ofdendrons, for those with a hydroxyl focal point. One dendrimer and one dendron, both bearing a sulfuratom close to the surface, scored best in the activity-toxicity relationship analysis and were chosen forresistance assays. No changes in the inhibitory and bactericidal capacity in the case of the dendron and onlya 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 ofbiofilm at concentrations over the minimum inhibitory concentration (MIC). SN 2046-2069 YR 2016 FD 2016-01-01 LK http://hdl.handle.net/10017/34040 UL http://hdl.handle.net/10017/34040 LA eng NO Ministerio de Economía y Empresa DS MINDS@UW RD 28-mar-2024