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拉氧头孢:一种可使β-内酰胺酶失活的氧杂β-内酰胺类抗生素。

Moxalactam: an oxa-beta-lactam antibiotic that inactivates beta-lactamases.

作者信息

Labia R

出版信息

Rev Infect Dis. 1982 Nov-Dec;4 Suppl:S529-35. doi: 10.1093/clinids/4.supplement_3.s529.

Abstract

Moxalactam, like cefoxitin, cefuroxime, and cefotaxime, shows little or no interaction with penicillinases. Resistance of moxalactam to cephalosporinases, however, appears to be considerably greater than that of these other recently discovered beta-lactam antibiotics. Moxalactam is a beta-lactamase inactivator and inactivates most of the cephalosporinases produced by gram-negative bacteria. The process of inactivation is specific and follows time-dependent or progressive kinetics, as is the case for a class of enzyme inhibitors called "suicide substrates." Moxalactam is the first beta-lactam antibiotic shown to possess this property of inactivation of beta-lactamases, a property that explains its excellent resistance to beta-lactamases.

摘要

羟羧氧酰胺菌素与头孢西丁、头孢呋辛和头孢噻肟一样,与青霉素酶几乎没有相互作用或无相互作用。然而,羟羧氧酰胺菌素对头孢菌素酶的耐药性似乎比其他这些最近发现的β-内酰胺类抗生素要高得多。羟羧氧酰胺菌素是一种β-内酰胺酶灭活剂,可灭活大多数革兰氏阴性菌产生的头孢菌素酶。灭活过程具有特异性,并遵循时间依赖性或渐进性动力学,一类称为“自杀底物”的酶抑制剂就是这种情况。羟羧氧酰胺菌素是第一种被证明具有灭活β-内酰胺酶这一特性的β-内酰胺类抗生素,这一特性解释了它对β-内酰胺酶的优异耐药性。

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