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2079-63821052021May17Antibiotics (Basel, Switzerland)Antibiotics (Basel)Insight on the Structure-to-Activity of Carbosilane Metallodendrimers in the Fight against Staphylococcus aureus Biofilms.58910.3390/antibiotics10050589Biofilm formation is a critical health concern, involved in most human bacterial infections. Combatting this mechanism, which increases resistance to traditional antibiotics and host immune defences, requires novel therapeutic approaches. The remarkable biocide activity and the monodispersity of carbosilane metallodendrimers make them excellent platforms to evaluate the impact of different structural parameters on the biological activity. In this work, we explore the influence of iminopyridine ring substituents on the antibacterial activity against planktonic and biofilm Staphylococcus aureus. New families of first-generation Ru(II) and Cu(II) metallodendrimers were synthesised and analysed, in comparison to the non-substituted counterparts. The results showed that the presence of methyl or methoxy groups in meta position to the imine bond decreased the overall positive charge on the metal ion and, subsequently, the activity against planktonic bacteria. However, it seemed a relevant parameter to consider for the prevention of biofilm formation, if they contribute to increasing the overall lipophilicity. An optimum balance of the charge and lipophilicity of the metallodrug, accomplished through structural design, will provide effective biocide agents against bacteria biofilms.LlamazaresCeliaCUniversity of Alcala, Department of Biomedicine and Biotechnology, 28805 Madrid, Spain.Sanz Del OlmoNataliaNUniversity of Alcala, Research Institute in Chemistry "Andrés M. del Río" (IQAR) and Faculty of Science, Department of Organic and Inorganic Chemistry, 28805 Madrid, Spain.SoliveriJuanJUniversity of Alcala, Department of Biomedicine and Biotechnology, 28805 Madrid, Spain.de la MataF JavierFJ0000-0003-0418-3935University of Alcala, Research Institute in Chemistry "Andrés M. del Río" (IQAR) and Faculty of Science, Department of Organic and Inorganic Chemistry, 28805 Madrid, Spain.Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), 28029 Madrid, Spain.University of Alcala, Institute Ramón y Cajal for Health Research (IRYCIS), 28034 Madrid, Spain.Copa-PatiñoJosé LuisJL0000-0002-2162-3907University of Alcala, Department of Biomedicine and Biotechnology, 28805 Madrid, Spain.García-GallegoSandraSUniversity of Alcala, Research Institute in Chemistry "Andrés M. del Río" (IQAR) and Faculty of Science, Department of Organic and Inorganic Chemistry, 28805 Madrid, Spain.Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), 28029 Madrid, Spain.University of Alcala, Institute Ramón y Cajal for Health Research (IRYCIS), 28034 Madrid, Spain.engCTQ2017-86224-PMinisterio de Economía y CompetitividadIMMUNOTHERCAN-CM B2017/BMD-3733Comunidad de MadridNANODENDMED-II B2017/BMD-3703Comunidad de MadridResearch Talent Attraction Program 2017-T2/IND-5243Comunidad de MadridSBPLY/17/180501/000358Junta de Comunidades de Castilla-La ManchaCIBER-BBNInstituto de Salud Carlos IIIBeatriz Galindo grant BG20/00231Spanish Ministry of UniversitiesProject CM/BG/2021-001Comunidad de Madrid and University of AlcalaJournal Article20210517
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