RESUMO
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.
Assuntos
Acetamidas/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Oxazolidinonas/química , Oxazolidinonas/farmacologia , Piridinas/química , Antibacterianos/química , Enterococcus/efeitos dos fármacos , Linezolida , Estrutura Molecular , Oxazolidinonas/síntese química , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-AtividadeRESUMO
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.
Assuntos
Antibacterianos/síntese química , Isoxazóis/síntese química , Oxazolidinonas/síntese química , Animais , Antibacterianos/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Feminino , Isoxazóis/farmacologia , Camundongos , Testes de Sensibilidade Microbiana/métodos , Oxazolidinonas/farmacologiaRESUMO
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.
