FLAVONOID BIOCIDES - STRUCTURE ACTIVITY RELATIONS OF FLAVONOID PHYTOALEXIN ANALOGS
FLAVONOID BIOCIDES - STRUCTURE ACTIVITY RELATIONS OF FLAVONOID PHYTOALEXIN ANALOGS
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DOI：
10.1016/0031-9422(89)85015-0
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发表时间：
1989-01-01
期刊：
影响因子：
3.8
通讯作者：
PRUNER, MS
中科院分区：
文献类型：
--
作者：
LAKS, PE;PRUNER, MS
合成了两组半合成的黄酮类植物防御素类似物，并对其亲脂性（RM）与抗真菌和抗菌活性进行了相关性研究。两种天然植物抗毒素，pisatin和maackiain，也在这些相同的条件下进行了测试，并确定了它们的RM。所观察到的结构/活性关系表明，这些类似物，和植物抗毒素，功能主要是作为解偶联剂的氧化磷酸化。相对酸度和羟基数是影响黄酮类化合物抑菌活性的主要因素。对于细菌屎链球菌，两组类似物的亲脂性和抗菌活性之间不存在相同的简单相关性，这意味着它们具有不同的作用模式。
Two sets of semisynthetic flavonoid phytoalexin analogues were synthesized and their lipophilicity (RM) correlated with their antifungal and antibacterial activity. Two natural pytoalexins, pisatin and maackiain, were also tested under these same conditions, and their RM''s determined. The observed structure/activity relationships suggest that these analogues, and the phytoalexins, function primarily as uncouplers of oxidative phosphorylation. The relative acidity and number of hydroxyl groups per molecule apear to be the main factors affecting the antifungal activity of flavonoids. With bacterium, Streptococcus faecium, there is not the same simple correlation between lipophilicity and antibacterial activity for the two sets of analogues, implying they have different models of action.