dc.creator | Cebrián, Rubén | es |
dc.creator | Lucas Rodríguez, Ricardo | es |
dc.creator | Fernández Cantos, María Victoria | es |
dc.creator | Slot, Koen | es |
dc.creator | Peñalver, Pablo | es |
dc.creator | Martínez García, Marta | es |
dc.creator | Párraga Leo, Antonio | es |
dc.creator | Paz Báñez, María Violante de | es |
dc.creator | García, Federico | es |
dc.creator | Kuipers, Oscar P. | es |
dc.creator | Morales, Juan Carlos | es |
dc.date.accessioned | 2023-04-18T13:50:09Z | |
dc.date.available | 2023-04-18T13:50:09Z | |
dc.date.issued | 2023 | |
dc.identifier.citation | Cebrián, R., Lucas Rodríguez, R., Fernández Cantos, M.V., Slot, K., Peñalver, P., Martínez García, M.,...,Morales, J.C. (2023). Synthesis and Antimicrobial Activity of Aminoalkyl Resveratrol Derivatives Inspired by Cationic Peptides. Journal of Enzyme Inhibition and Medicinal Chemistry, 38 (1), 267-281. https://doi.org/10.1080/14756366.2022.2146685. | |
dc.identifier.issn | 1475-6366 | es |
dc.identifier.issn | 1475-6374 | es |
dc.identifier.uri | https://hdl.handle.net/11441/144592 | |
dc.description.abstract | Antimicrobial resistance is a global concern, far from being resolved. The need of new drugs against new targets is imminent. In this work, we present a family of aminoalkyl resveratrol derivatives with antibacterial activity inspired by the properties of cationic amphipathic antimicrobial peptides. Surprisingly, the newly designed molecules display modest activity against aerobically growing bacteria but show surprisingly good antimicrobial activity against anaerobic bacteria (Gram-negative and Gram-positive) suggesting specificity towards this bacterial group. Preliminary studies into the action mechanism suggest that activity takes place at the membrane level, while no cross-resistance with traditional antibiotics is observed. Actually, some good synergistic relations with existing antibiotics were found against Gram-negative pathogens. However, some cytotoxicity was observed, despite their low haemolytic activity. Our results show the importance of the balance between positively charged moieties and hydrophobicity to improve antimicrobial activity, setting the stage for the design of new drugs based on these molecules. | es |
dc.description.sponsorship | Junta de Andalucía FQM-7316 | es |
dc.description.sponsorship | Dutch Research Council NWA.1228.191.006 | es |
dc.description.sponsorship | National Institute of Allergy and Infectious Diseases CL03T12C32 | es |
dc.format | application/pdf | es |
dc.format.extent | 15 p. | es |
dc.language.iso | eng | es |
dc.publisher | Taylor & Francis | es |
dc.relation.ispartof | Journal of Enzyme Inhibition and Medicinal Chemistry, 38 (1), 267-281. | |
dc.rights | Atribución 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | * |
dc.subject | Aminoalkyl | es |
dc.subject | Anaerobic bacteria | es |
dc.subject | Antimicrobial | es |
dc.subject | Haemolysis | es |
dc.subject | Membrane permeabilization | es |
dc.subject | Resveratrol | es |
dc.subject | Synergism | es |
dc.subject | Toxicity | es |
dc.title | Synthesis and Antimicrobial Activity of Aminoalkyl Resveratrol Derivatives Inspired by Cationic Peptides | es |
dc.type | info:eu-repo/semantics/article | es |
dcterms.identifier | https://ror.org/03yxnpp24 | |
dc.type.version | info:eu-repo/semantics/publishedVersion | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica | es |
dc.relation.projectID | FQM-7316 | es |
dc.relation.projectID | NWA.1228.191.006 | es |
dc.relation.projectID | CL03T12C32 | es |
dc.relation.publisherversion | https://dx.doi.org/10.1080/14756366.2022.2146685 | es |
dc.identifier.doi | 10.1080/14756366.2022.2146685 | es |
dc.journaltitle | Journal of Enzyme Inhibition and Medicinal Chemistry | es |
dc.publication.volumen | 38 | es |
dc.publication.issue | 1 | es |
dc.publication.initialPage | 267 | es |
dc.publication.endPage | 281 | es |
dc.contributor.funder | Junta de Andalucía | es |
dc.contributor.funder | Dutch Research Council (NWA). Paises Bajos | es |
dc.contributor.funder | National Institute of Allergy and Infectious Diseases (NIAID). USA | es |