RESUMEN
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.
Asunto(s)
Cefalosporinas/síntesis química , Penicilinas/síntesis química , Administración Oral , Animales , Infecciones Bacterianas/tratamiento farmacológico , Cefalosporinas/administración & dosificación , Cefalosporinas/metabolismo , Cefalosporinas/farmacología , Inyecciones Subcutáneas , Masculino , Ratones , Pruebas de Sensibilidad Microbiana , Penicilinas/administración & dosificación , Penicilinas/metabolismo , Penicilinas/farmacología , Relación Estructura-ActividadRESUMEN
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.