RESUMEN
A series of pyrrolopyridine-substituted oxazolidinones containing various C-5 acetamide isosteres was synthesized and the structure-antibacterial activity relationships determined against a representative panel of susceptible and resistant Gram-positive bacteria.
Asunto(s)
Acetamidas/química , Antibacterianos/síntesis química , Antibacterianos/farmacología , Oxazolidinonas/química , Oxazolidinonas/farmacología , Piridinas/química , Antibacterianos/química , Enterococcus/efectos de los fármacos , Linezolid , Estructura Molecular , Oxazolidinonas/síntesis química , Staphylococcus aureus/efectos de los fármacos , Relación Estructura-ActividadRESUMEN
A series of oxazolidinone antibacterial agents containing a 5-substituted isoxazol-3-yl moiety were synthesized via a nitrile oxide [3+2] dipolar cycloaddition reaction. These compounds were screened against a panel of susceptible and resistant Gram-positive organisms. Several analogs from this series were comparable to or more potent than linezolid in vitro.
Asunto(s)
Antibacterianos/síntesis química , Isoxazoles/síntesis química , Oxazolidinonas/síntesis química , Animales , Antibacterianos/farmacología , Evaluación Preclínica de Medicamentos/métodos , Femenino , Isoxazoles/farmacología , Ratones , Pruebas de Sensibilidad Microbiana/métodos , Oxazolidinonas/farmacologíaRESUMEN
A novel series of oxazolidinones containing a pyrroloaryl substituent was synthesized and screened against a representative panel of susceptible and resistant Gram-positive bacteria. Several members of this series were found to have antibacterial activity comparable to or better than linezolid.
