Spirocyclopropyl beta-lactams as mechanism-based inhibitors of serine beta-lactamases. Synthesis by rhodium-catalyzed cyclopropanation of 6-diazopenicillanate sulfone.
J Med Chem
; 46(13): 2569-71, 2003 Jun 19.
Article
em En
| MEDLINE
| ID: mdl-12801220
ABSTRACT
Class A-class C mechanism-based beta-lactamase inhibitors were designed on the basis of the intermediacy of an oxycarbenium species capable of cross-linking with amino acids residues in the active site. Penams 24 and 27 were very potent against AmpC in vitro. The MIC values of 24 in combination with piperacillin against class A and class C producing organisms showed improvement over clinically used tazobactam.
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Coleções:
01-internacional
Contexto em Saúde:
3_ND
Base de dados:
MEDLINE
Assunto principal:
Ródio
/
Serina
/
Compostos de Espiro
/
Proteínas de Bactérias
/
Sulbactam
/
Ciclopropanos
/
Beta-Lactamas
/
Compostos de Diazônio
/
Inibidores Enzimáticos
/
Inibidores de beta-Lactamases
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2003
Tipo de documento:
Article