RESUMO

The triflates and pivalates of 3 alpha-hydroxymethyl-6-substituted-2,2-dimethylpenam sulfones 3, 5; methyl and benzyl 6-substituted penicillanates 6-9 and 3-exo-methylene-6-substituted-2,2-dimethylpenam sulfone 4 were synthesized. These novel compounds were evaluated as elastase inhibitors using porcine pancreatic elastase. The effects that structural modifications of substituents on C-3 and C-6 in the penam nucleus have on elastase activity were examined and several similarities and distinctions were identified when compared to the reported penicillin esters and amides elastase inhibitors.

Assuntos

Elastase Pancreática/antagonistas & inibidores , Sulbactam/análogos & derivados , Sulfonas/síntese química , Animais , Estrutura Molecular , Relação Estrutura-Atividade , Sulbactam/síntese química , Sulbactam/farmacologia , Sulfonas/farmacologia , Suínos