| Autor: |
Suay-García B; ESI International Chair@CEU-UCH, Departamento de Matemáticas, Física y Ciencias Tecnológicas, Universidad Cardenal Herrera-CEU, CEU Universities San Bartolomé 55, 46115 Alfara del Patriarca, Valencia, Spain., Bueso-Bordils JI; Departamento de Farmacia, Universidad Cardenal Herrera-CEU, CEU Universities C/Ramón y Cajal s/n, 46115 Alfara del Patriarca, Valencia, Spain., Antón-Fos G; Departamento de Farmacia, Universidad Cardenal Herrera-CEU, CEU Universities C/Ramón y Cajal s/n, 46115 Alfara del Patriarca, Valencia, Spain., Pérez-Gracia MT; Departamento de Farmacia, Universidad Cardenal Herrera-CEU, CEU Universities C/Ramón y Cajal s/n, 46115 Alfara del Patriarca, Valencia, Spain., Falcó A; ESI International Chair@CEU-UCH, Departamento de Matemáticas, Física y Ciencias Tecnológicas, Universidad Cardenal Herrera-CEU, CEU Universities San Bartolomé 55, 46115 Alfara del Patriarca, Valencia, Spain., Alemán-López P; Departamento de Farmacia, Universidad Cardenal Herrera-CEU, CEU Universities C/Ramón y Cajal s/n, 46115 Alfara del Patriarca, Valencia, Spain. |
| Abstrakt: |
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. |
