Efficacy of Piperacillin Combined with the Penem β-Lactamase Inhibitor BLI-489 in Murine Models of Systemic Infection

Efficacy of Piperacillin Combined with the Penem β-Lactamase Inhibitor BLI-489 in Murine Models of Systemic Infection
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哌拉西林联合培南 β-内酰胺酶抑制剂 BLI-489 在小鼠全身感染模型中的疗效

DOI:
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发表时间:
2009
影响因子:
4.9
通讯作者:
P. Bradford
P. Bradford
中科院分区:
医学2区
文献类型:
--
作者:
P. Petersen;C. H. Jones;A. Venkatesan;P. Bradford

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在小鼠中使用急性致死性全身感染来测定哌拉西林与青霉烯抑制剂BLI-489组合的体内功效。根据不同比例的初步结果,发现8:1的给药比例对于保持增强的功效是最佳的。以8:1的比例给药的克拉霉素-BLI-489对由A类(包括超广谱β-内酰胺酶)、C类(AmpC)和D类β-内酰胺酶表达病原体引起的鼠感染有效。
ABSTRACT The in vivo efficacy of piperacillin in combination with the penem inhibitor BLI-489 was determined using acute lethal systemic infections in mice. On the basis of preliminary results with various ratios, a dosing ratio of 8:1 was found to be optimal for retention of enhanced efficacy. Piperacillin-BLI-489 dosed at an 8:1 ratio was efficacious against murine infections caused by class A (including extended-spectrum β-lactamases), class C (AmpC), and class D β-lactamase-expressing pathogens.
带有三环杂环的 6-亚甲基青霉烯作为广谱 β-内酰胺酶抑制剂的结构-活性关系:晶体结构显示出意外的 1,4-硫氮杂卓中间体结合。
DOI: 10.1021/jm049680x
发表时间: 2004
期刊: Journal of medicinal chemistry.
影响因子: --
作者:
Venkatesan,AranapakamM;Gu,Yansong;DosSantos,Osvaldo;Abe,Takao;Agarwal,Atul;Yang,Youjun;Petersen,PeterJ;Weiss,WilliamJ;Mansour,TarekS;Nukaga,Michiyoshi;Hujer,AndreaM;Bonomo,RobertA;Knox,JamesR
通讯作者: Knox,JamesR