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Meridianin D Analogues Display Antibiofilm Activity against MRSA and Increase Colistin Efficacy in Gram-Negative Bacteria
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2018-05-25 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00161
William M. Huggins 1 , William T. Barker 1 , James T. Baker 1 , Nicholas A. Hahn 1 , Roberta J. Melander 1 , Christian Melander 1
Affiliation  

In the last 30 years, development of new classes of antibiotics has slowed, increasing the necessity for new options to treat multidrug resistant bacterial infections. Development of antibiotic adjuvants that increase the effectiveness of currently available antibiotics is a promising alternative approach to classical antibiotic development. Reports of the ability of the natural product meridianin D to modulate bacterial behavior have been rare. Herein, we describe the ability of meridianin D to inhibit biofilm formation of methicillin-resistant Staphylococcus aureus (MRSA) and to increase the potency of colistin against colistin-resistant and sensitive Gram-negative bacteria. Analogues were identified that are capable of inhibiting and dispersing MRSA biofilms and lowering the colistin MIC to below the CLSI breakpoint against Acinetobacter baumannii, Klebsiella pneumoniae, and Escherichia coli.

中文翻译:

Meridianin D类似物显示抗MRSA的抗生物膜活性并增加革兰氏阴性细菌的共利斯汀功效。

在过去的30年中,新型抗生素的开发速度减慢,增加了治疗耐多药细菌感染的新选择的必要性。抗生素佐剂的开发增加了当前可用抗生素的有效性,是经典抗生素开发的一种有前途的替代方法。天然产物子午线D调节细菌行为的能力的报道很少。在这里,我们描述了子午线D抑制耐甲氧西林金黄色葡萄球菌生物膜形成的能力(MRSA),并提高大肠菌素对大肠菌素耐药和敏感的革兰氏阴性细菌的效力。类似物被鉴定为能够抑制和分散MRSA生物膜并降低大肠埃希菌鲍曼不动杆菌肺炎克雷伯菌大肠埃希菌的MIC到CLSI断裂点以下。
更新日期:2018-05-25
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