RESUMO
The synthesis of a new series of 1beta-methylcarbapenems having methoxyimine and substituted sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. A particular compound (IIIc) having methylaminosulfonamide moiety showed the most potent antibacterial activity.
Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Carbapenêmicos/síntese química , Carbapenêmicos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-AtividadeRESUMO
The synthesis of a new series of 1beta-methylcarbapenems having a 5-(1,2-disubstituted ethyl) pyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the pyrrolidine ring was investigated. A particular compound IIIf having a 1-methoxyimino-2-carbamoylethyl substituted moiety showed the most potent antibacterial activity.
Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Carbapenêmicos , Testes de Sensibilidade Microbiana , Relação Estrutura-AtividadeRESUMO
The synthesis of a new series of 1beta-methylcarbapenems containing the substituted thiazolidinopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituent on the thiazolidine ring was investigated.A particular compound (18 c) having a 2-amide substituted thiazolidine moiety showed the most potent antibacterial activity.