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Synthesis and antifungal activity of 2,4-dihydroxy-5-methylphenyl ethanone derivatives against phytopathogenic fungi in vitro
Phytochemistry Letters ( IF 1.3 ) Pub Date : 2023-12-09 , DOI: 10.1016/j.phytol.2023.11.008
Lin Jia , Cui-Ping Zhang , Yi Zhu , Chun-Yan Zhao , Zeng-Hui Han , Dong-Bao Hu , Wei Shi

In an endeavor to pinpoint the structural constituents vital for the biological activity of 2,4-dihydroxy-5-methylphenyl ethanone, a series of its ether derivatives was synthesized and examined for their antifungal activities against five notable phytopathogenic fungi. The bioassay revealed that compounds 2, 3a, 3g, 3j and 3k manifested a broad spectrum of antifungal efficacy. Notably, compound 3g was identified as especially potent, with IC50 values ranging from 16.52 to 37.52 μg/mL, outperforming the standard thiabendazole. The data underscore compound 3g as a prospective candidate for the development of an innovative antifungal agent. A comprehensive structure-activity relationship (SAR) study of the acetophenones was also conducted.



中文翻译:

2,4-二羟基-5-甲基苯基乙酮衍生物的合成及其体外抗真菌活性

为了查明对 2,4-二羟基-5-甲基苯基乙酮生物活性至关重要的结构成分,合成了一系列其醚衍生物,并检查了它们对五种著名植物病原真菌的抗真菌活性。生物测定表明,化合物2、3a3g3j3k表现出广谱的抗真菌功效。值得注意的是,化合物3g被认为特别有效,IC 50值范围为 16.52 至 37.52  μg /mL,优于标准噻菌灵。该数据强调化合物3g作为开发创新抗真菌剂的潜在候选者。还对苯乙酮进行了全面的构效关系(SAR)研究。

更新日期:2023-12-09
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