Novel cajaninstilbene acid derivatives as antibacterial agents
Novel cajaninstilbene acid derivatives as antibacterial agents
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DOI：
10.1016/j.ejmech.2015.06.008
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发表时间：
2015-07-15
影响因子：
6.7
通讯作者：
Chen, Wei-Min
中科院分区：
文献类型：
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作者：
Geng, Zhi-Zhong;Zhang, Jian-Jun;Chen, Wei-Min
寻找具有新型结构支架的新型抗菌剂以对抗耐药病原体是一项紧迫的任务。木犀草酸是从木豆叶中分离得到的一种具有抗菌活性的化合物。本研究设计合成了一系列木犀草酸的衍生物。评价了这些化合物对革兰氏阴性菌和革兰氏阳性菌以及9株耐甲氧西林金黄色葡萄球菌(MRSA)的抑菌活性，并讨论了相关的构效关系。分析表明，一些合成的木犀草酸衍生物对革兰氏阳性细菌和耐甲氧西林金黄色葡萄球菌具有很强的抗菌活性。其中，5b、5c、5j和5k的抗菌活性优于阳性对照化合物。四甲基偶氮唑盐比色试验结果表明，活性化合物具有较低的细胞毒性。(C)2015年爱思唯尔·马森公司。版权所有。
Discovery of novel antibacterial agents with new structural scaffolds that combat drug-resistant pathogens is an urgent task. Cajaninstilbene acid, which is isolated from pigeonpea leaves, has shown antibacterial activity. In this study, a series of cajaninstilbene acid derivatives were designed and synthesized. The antibacterial activities of these compounds against gram-negative and gram-positive bacteria, as well as nine strains of methicillin-resistant staphylococcus aureus (MRSA) bacteria are evaluated, and the related structure-activity relationships are discussed. Assays suggest that some of the synthetic cajaninstilbene acid derivatives exhibit potent antibacterial activity against gram-positive bacterial strains and MRSA. Among these compounds, 5b, 5c, 5j and 5k show better antibacterial activity than the positive control compounds. The results of MTT assays illustrate the low cytotoxicity of the active compounds. (C) 2015 Elsevier Masson SAS. All rights reserved.