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Synthesis of quinolones and zwitterionic quinolonate derivatives with broad-spectrum antibiotic activity

Título : Synthesis of quinolones and zwitterionic quinolonate derivatives with broad-spectrum antibiotic activity
Autor : Suay García, Beatriz
Bueso Bordils, José Ignacio
Antón Fos, Gerardo Manuel
Pérez Gracia, María Teresa.
Falcó Montesinos, Antonio
Alemán López, Pedro
Materias: Bacteria - Drug resistance - Mathematical models.Biología molecular - Modelos matemáticos.Molecular biology - Mathematical models.Topología - Aplicaciones en bioquímica.Bacterias - Resistencia a los medicamentos - Modelos matemáticos.Quinolonas - Modelos matemáticos.Quinolone antibacterial agents - Mathematical models.Antibióticos - Modelos matemáticos.Antibiotics - Mathematical models.Topology in biochemistry.
Editorial : MDPI
Citación : Suay-García, B., Bueso-Bordils, J. I., Antón-Fos, G., Pérez-Gracia, M. T., Falcó, A. & Alemán-López, P. (2022). Synthesis of quinolones and zwitterionic quinolonate derivatives with broad-spectrum antibiotic activity. Pharmaceuticals, vol. 15, i. 7 (01 jul.), art. 818. DOI: https://doi.org/10.3390/ph15070818
Resumen : Quinolones are one of the most extensively used therapeutic families of antibiotics. However, the increase in antibiotic-resistant bacteria has rendered many of the available compounds useless. After applying our prediction model of activity against E. coli to a library of 1000 quinolones, two quinolones were selected to be synthesized. Additionally, a series of zwitterionic quinolonates were also synthesized. Quinolones and zwitterionic quinolonates were obtained by coupling the corresponding amine with reagent 1 in acetonitrile. Antibacterial activity was assessed using a microdilution method. All the compounds presented antibacterial activity, especially quinolones 2 and 3, selected by the prediction model, which had broad-spectrum activity. Furthermore, a new type of zwitterionic quinolonate with antibacterial activity was found. These compounds can lead to a new line of antimicrobials, as the structures, and, therefore, their properties, are easily adjustable in the amine in position 4 of the pyridine ring.
Descripción : Este artículo se encuentra disponible en la siguiente URL: https://www.mdpi.com/1424-8247/15/7/818
Este artículo de investigación pertenece al número especial "Novel Antibacterial Agents 2022".
URI : http://hdl.handle.net/10637/14213
Derechos: http://creativecommons.org/licenses/by/4.0/deed.es
ISSN : 1424-8247 (Electrónico)
Idioma: es
Fecha de publicación : 1-jul-2022
Centro : Universidad Cardenal Herrera-CEU
Aparece en las colecciones: Dpto. Farmacia





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