头孢菌素-3'-重氮亚氨基二氢氧化物的合成：β-内酰胺酶激活的生物膜分散型 NO 供体前药。
Synthesis of cephalosporin-3'-diazeniumdiolates: biofilm dispersing NO-donor prodrugs activated by β-lactamase.
机构信息
School of Chemistry, University of Wollongong, NSW 2522, Australia.
出版信息
Chem Commun (Camb). 2013 May 25;49(42):4791-3. doi: 10.1039/c3cc40869h.
Use of biofilm dispersing NO-donor compounds in combination with antibiotics has emerged as a promising new strategy for treating drug-resistant bacterial biofilm infections. This paper details the synthesis and preliminary evaluation of six cephalosporin-3'-diazeniumdiolates as biofilm-targeted NO-donor prodrugs. Each of the compounds is shown to selectively release NO following reaction with the bacteria-specific enzyme β-lactamase and to trigger dispersion of Pseudomonas aeruginosa biofilms in vitro.
使用生物膜分散型一氧化氮供体化合物与抗生素联合治疗耐药性细菌生物膜感染已成为一种有前途的新策略。本文详细介绍了六种头孢菌素-3'-偶氮氮醇盐作为靶向生物膜的一氧化氮供体前药的合成和初步评价。结果表明，每种化合物在与细菌特异性酶β-内酰胺酶反应后均能选择性地释放一氧化氮，并能触发铜绿假单胞菌生物膜的体外分散。
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