Inhibition of OXA-1 beta-lactamase by penems.
Antimicrob Agents Chemother
; 52(9): 3135-43, 2008 Sep.
Article
em En
| MEDLINE
| ID: mdl-18559643
ABSTRACT
The partnering of a beta-lactam with a beta-lactamase inhibitor is a highly effective strategy that can be used to combat bacterial resistance to beta-lactam antibiotics mediated by serine beta-lactamases (EC 3.2.5.6). To this end, we tested two novel penem inhibitors against OXA-1, a class D beta-lactamase that is resistant to inactivation by tazobactam. The K(i) of each penem inhibitor for OXA-1 was in the nM range (K(i) of penem 1, 45 +/- 8 nM; K(i) of penem 2, 12 +/- 2 nM). The first-order rate constant for enzyme and inhibitor complex inactivation of penems 1 and 2 for OXA-1 beta-lactamase were 0.13 +/- 0.01 s(-1) and 0.11 +/- 0.01 s(-1), respectively. By using an inhibitor-to-enzyme ratio of 11, 100% inactivation was achieved in
Texto completo:
1
Coleções:
01-internacional
Contexto em Saúde:
3_ND
Base de dados:
MEDLINE
Assunto principal:
Compostos Bicíclicos com Pontes
/
Inibidores Enzimáticos
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Escherichia coli
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Inibidores de beta-Lactamases
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Compostos Heterocíclicos
Idioma:
En
Revista:
Antimicrob Agents Chemother
Ano de publicação:
2008
Tipo de documento:
Article