In vitro activity of BAL30072 against Burkholderia pseudomallei.
In vitro activity of BAL30072 against Burkholderia pseudomallei.
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DOI：
10.1016/j.ijantimicag.2011.03.019
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发表时间：
2011-08
影响因子：
10.8
通讯作者：
Schweizer HP
中科院分区：
文献类型：
--
作者：
Mima T;Kvitko BH;Rholl DA;Page MG;Desarbre E;Schweizer HP
假性伯克霍尔德菌是一种内在耐药的B类优先病原体，是类鼻疽病的病原。假芽孢杆菌感染的治疗是两期和漫长的，以对抗疾病的急性和慢性阶段。急性期治疗最好包括静脉注射头孢菌素（头孢他啶）或碳青霉烯（亚胺培南或美罗培南）。在这项研究中，抗b。研究了一种新型单磺胺药BAL30072对实验室菌株1026b和1710b、几种等基因突变衍生物以及来自泰国的临床和环境假马莱杆菌菌株的药效。93%以上菌株的最低抑菌浓度（mic）在0.004 ~ 0.016 μg/mL范围内。对实验室菌株1026b， BAL30072的MIC为0.008 μg/mL，与头孢他啶1.5 μg/mL、亚胺培南0.5 μg/mL、美罗培南1 μg/mL相当。时间-杀伤曲线显示，BAL30072具有快速杀菌作用，2 h内可杀灭50%以上的细菌。BAL30072的活性不受外排的显著影响，它只是PenA β-内酰胺酶的边缘底物，其活性不依赖于马来菌素的产生和运输，也不依赖于脓螯素的运输能力。综上所述，BAL30072与头孢他啶、美罗培南和亚胺培南相比，具有较好的体外抑菌活性，且具有快速杀菌作用。
Burkholderia pseudomallei is an intrinsically antibiotic-resistant Category B priority pathogen and the aetiological agent of melioidosis. Treatment of B. pseudomallei infection is biphasic and lengthy in order to combat the acute and chronic phases of the disease. Acute-phase treatment preferably involves an intravenous cephalosporin (ceftazidime) or a carbapenem (imipenem or meropenem). In this study, the anti-B. pseudomallei efficacy of a new monosulfactam, BAL30072, was tested against laboratory strains 1026b and 1710b and several isogenic mutant derivatives as well as a collection of clinical and environmental B. pseudomallei strains from Thailand. More than 93% of the isolates had minimal inhibitory concentrations (MICs) in the range 0.004–0.016 μg/mL. For the laboratory strain 1026b, the MIC of BAL30072 was 0.008 μg/mL, comparable with the MICs of 1.5 μg/mL for ceftazidime, 0.5 μg/mL for imipenem and 1 μg/mL for meropenem. Time–kill curves revealed that BAL30072 was rapidly bactericidal, killing >99% of bacteria in 2 h. BAL30072 activity was not significantly affected by efflux, it was only a marginal substrate of PenA β-lactamase, and activity was independent of malleobactin production and transport and the ability to transport pyochelin. In summary, BAL30072 has superior in vitro activity against B. pseudomallei compared with ceftazidime, meropenem or imipenem and it is rapidly bactericidal.
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影响因子：
3.2
作者：
DeShazer, D;Brett, PJ;Woods, DE
通讯作者：
Woods, DE
影响因子：
5.2
作者：
Mushtaq, Shazad;Warner, Marina;Livermore, David
通讯作者：
Livermore, David
影响因子：
3.2
作者：
Alice, AF;López, CS;Crosa, JH
通讯作者：
Crosa, JH
DOI：
10.1073/pnas.78.7.4256
发表时间：
1981-01-01
期刊：
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES
影响因子：
--
作者：
COX, CD;RINEHART, KL;COOK, JC
通讯作者：
COOK, JC
影响因子：
3.8
作者：
Trunck LA;Propst KL;Wuthiekanun V;Tuanyok A;Beckstrom-Sternberg SM;Beckstrom-Sternberg JS;Peacock SJ;Keim P;Dow SW;Schweizer HP
通讯作者：
Schweizer HP