RESUMO
A number of orally active cephalosporins and penicillins with interesting biological activity were synthesized. Two of these, 7-[[[3,4-(methylenedioxy)phenyl]glycyl]amino]deacetoxycephalosporanic acid and 7-[[2-(2,3-dihydro-5-benzofuranyl)glycyl]amino]deacetoxycephalosporanic acid were considerably more active than cephalexin both in vitro and in vivo against staphylococcal and streptococcal infections.
Assuntos
Cefalosporinas/síntese química , Penicilinas/síntese química , Administração Oral , Animais , Infecções Bacterianas/tratamento farmacológico , Cefalosporinas/administração & dosagem , Cefalosporinas/metabolismo , Cefalosporinas/farmacologia , Injeções Subcutâneas , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Penicilinas/administração & dosagem , Penicilinas/metabolismo , Penicilinas/farmacologia , Relação Estrutura-AtividadeRESUMO
Three cephalosporin derivatives were prepared from 1,4-dihydro-4-oxypyridine-1-acetic acid. These were the 7-aminocephalosporanic acid (7-ACA) derivative and the compounds with 5-methyl-1,3,4-thiadiazol-2-thiol and 1-methyl-1,2,3,4-tetrazole-5-thiol at C-3 of the cephalosporin nucleus. The antibacterial activity of the 7-ACA derivative was comparable to cephalothin, and that of the other two derivatives was comparable to cefazolin. The 7-ACA derivative, compared to cephalothin, was significantly less metabolized, was less protein bound, and had a longer half life.