Synthesis and antimicrobial activity of amide derivatives of polyether antibiotic-salinomycin
Synthesis and antimicrobial activity of amide derivatives of polyether antibiotic-salinomycin
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DOI：
10.1016/j.bmcl.2012.05.081
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发表时间：
2012-07-15
影响因子：
2.7
通讯作者：
Brzezinski, Bogumil
中科院分区：
文献类型：
--
作者：
Huczynski, Adam;Janczak, Jan;Brzezinski, Bogumil
本文首次介绍了聚醚类抗生素-盐碱霉素八种酰胺类衍生物的直接合成方法。用x射线衍射测定了烯丙酰胺（3a）的结构。盐霉素及其酰胺衍生物对典型革兰氏阳性球菌、革兰氏阴性杆状菌和酵母样生物，以及一系列耐甲氧西林金黄色葡萄球菌和甲氧西林敏感金黄色葡萄球菌的体外抗菌活性进行了筛选。研究发现，盐霉素酰胺具有广泛的活性，从256 μ g/mL时的无活性到MIC为2 μ g/mL时的活性，与盐霉素相当。结果发现，苯酰胺（3b）是抗革兰氏阳性菌、MRSA和MSSA活性最高的盐霉素衍生物。(C) 2012 Elsevier Ltd.版权所有。
For the first time a direct and practical approach to the synthesis of eight amide derivatives of polyether antibiotic-salinomycin is described. The structure of allyl amide (3a) has been determined using X-ray diffraction. Salinomycin and its amide derivatives have been screened for their in vitro antimicrobial activity against the typical Gram-positive cocci, Gram-negative rods and yeast-like organisms, as well as against a series of clinical isolates of methicillin-resistant Staphylococcus aureus and methicillin-sensitive S. aureus. Amides of salinomycin have been found to show a wide range of activities, from inactive at 256 mu g/mL to active with MIC of 2 mu g/mL, comparable with salinomycin. As a result, phenyl amide (3b) was found to be the most active salinomycin derivative against Gram-positive bacteria, MRSA and MSSA. (C) 2012 Elsevier Ltd. All rights reserved.