丹皮酚及百里酚磺酸酯类衍生物的合成及其抑菌活性

Synthesis of Paeonol and Thymol Sulfonate Derivatives and Their Antifun gal Activities

[目的]寻找较高抑菌活性的酚类化合物。[方法]采用菌丝生长速率法测试了丹皮酚和百里酚磺酸酯类衍生物的抑菌活性。[结果]在50 mg/L时,丹皮酚(1)衍生物4a~4n对供试病原菌表现出较好的抑制活性,部分表现出比阳性对照百菌清更高的抑制活性。而百里酚(2)衍生物5a~5n抑菌活性较低,酚羟基对于百里酚维持其高的抑菌活性十分关键。[结论]同属于酚类化合物,但酚羟基对于丹皮酚和百里酚抑菌活性的影响却大不相同,该研究为开发高效、低毒的新型杀菌剂提供理论参考。

[Aims] This study aims to search for phenolic derivatives with high antifungal activities. [Methods] Using paeonol and thymol as lead compounds, two series of novel phenolic derivatives 4a-4n and 5a-5n were synthesized.And these compounds were screened for antifungal activities against ten phytopathogenic fungi in vitro by using the mycelial growth rate method at the concentration of 50 mg/L. [Results] Generally, the compounds 4a-4n showed more antifungal activities against tested phytopathogenic fungi, some of which were even better than that of chlorothalonil, a commercially available agricultural fungicide. However, It is worth mentioning that the corresponding antifungal activities of 5a-5n synthesized from thymol(2) decreased sharply compared with 2, which indicated that hydroxyl group played a significant role in the antifungal activity for lead compound thymol. [Conclusions] Though paeonol and thymol are both simple phenolic compounds, the hydroxyl group played a different role in their antifungal activity,which provides a good guidance for further study of the phenolic derivatives to discovery potential antifungal agents with high efficacy, low toxicity as well as safety to non-target organisms.