Artículo
Synthesis and Antimicrobial Activity of Aminoalkyl Resveratrol Derivatives Inspired by Cationic Peptides
Autor/es | Cebrián, Rubén
Lucas Rodríguez, Ricardo Fernández Cantos, María Victoria Slot, Koen Peñalver, Pablo Martínez García, Marta Párraga Leo, Antonio Paz Báñez, María Violante de García, Federico Kuipers, Oscar P. Morales, Juan Carlos |
Departamento | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica |
Fecha de publicación | 2023 |
Fecha de depósito | 2023-04-18 |
Publicado en |
|
Resumen | 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 ... 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. |
Agencias financiadoras | Junta de Andalucía Dutch Research Council (NWA). Paises Bajos National Institute of Allergy and Infectious Diseases (NIAID). USA |
Identificador del proyecto | FQM-7316
NWA.1228.191.006 CL03T12C32 |
Cita | 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. |
Ficheros | Tamaño | Formato | Ver | Descripción |
---|---|---|---|---|
Synthesis and antimicrobial ... | 3.225Mb | [PDF] | Ver/ | |