Inhibition of OXA-1 beta-lactamase by penems.
Antimicrob Agents Chemother
; 52(9): 3135-43, 2008 Sep.
Article
en 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
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Compuestos Bicíclicos con Puentes
/
Inhibidores Enzimáticos
/
Escherichia coli
/
Inhibidores de beta-Lactamasas
/
Compuestos Heterocíclicos
Idioma:
En
Revista:
Antimicrob Agents Chemother
Año:
2008
Tipo del documento:
Article
País de afiliación:
Estados Unidos