1.
Bioorg Med Chem Lett
; 10(9): 847-51, 2000 May 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-10853645
RESUMO
A series of 2-substituted-7-(alkylidene)cephalosporin sulfones were prepared and evaluated as beta-lactamase inhibitors. Compound 11c showed excellent activity as an inhibitor of the class C beta-lactamase derived from Enterobacter cloacae, strain P99.
Assuntos
Alcenos/síntese química , Cefalosporinas/síntese química , Inibidores Enzimáticos/síntese química , Inibidores de beta-Lactamases , Alcenos/farmacologia , Cefalosporinas/farmacologia , Enterobacter cloacae/efeitos dos fármacos , Enterobacter cloacae/enzimologia , Inibidores Enzimáticos/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/enzimologia , Relação Estrutura-Atividade , beta-Lactamases
2.
Bioorg Med Chem Lett
; 9(14): 1997-2002, 1999 Jul 19.
Artigo
em Inglês
| MEDLINE
| ID: mdl-10450969
RESUMO
Penicillin sulfones, which structurally incorporate both a 6-position alkylidene substituent and a 2'beta substituent, have been synthesized and evaluated as inhibitors of class C and class A serine beta-lactamases. Incorporation of the 2'beta-substituent generally improves inhibitory activity. Substituents that improve transport across the bacterial cell membrane have also been incorporated.
