RESUMO
The synthesis of a new series of 1beta-methylcarbapenems having cyclic sulfonamide moieties is described. Their in-vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of a substituent on the pyrrolidine ring was investigated. One particular compound IIIe having a [1,2,5]thiadiazolidin 1,1-dioxide moiety showed the most potent antibacterial activity.
Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Carbapenêmicos/síntese química , Viabilidade Microbiana/efeitos dos fármacos , Sulfonamidas/síntese química , Antibacterianos/química , Avaliação Pré-Clínica de Medicamentos , Imipenem/farmacologia , Meropeném , Estrutura Molecular , Relação Estrutura-Atividade , Tienamicinas/farmacologiaRESUMO
The synthesis of a new series of 1beta-methylcarbapenems having cyclic sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. A particular compound (IIIi) having 2-methyl-[1,2,6]thiadiazinan-1,1-dioxide moiety showed the most potent antibacterial activity.