Design, synthesis, and bioactivity evaluation of novel thiochromanone derivatives containing an oxime or oxime ether moiety,Journal of Heterocyclic Chemistry

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Design, synthesis, and bioactivity evaluation of novel thiochromanone derivatives containing an oxime or oxime ether moiety
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-07-05 , DOI: 10.1002/jhet.4338
Lu Yu ₁ , Lingling Xiao ₁ , Jiyan Chi ₁ , Zhangfei Tang ₁ , Jie Li ₁ , Shuming Tan ₁ , Pei Li _{1,

2}

Affiliation

In this study, using botanical active component thiochromanone as the lead compound, a series of novel thiochromanone derivatives containing an oxime or oxime ether moiety were designed and synthesized. The half-maximal effective concentration (EC₅₀) values of compound 4a against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas oryzae pv. oryzicolaby (Xoc), and Xanthomonas axonopodis pv. citri (Xac) were 6, 10, and 15 μg/ml, respectively, which were superior to those of Bismerthiazol and Thiodiazole-copper. Meanwhile, compound 4a also revealed better antifungal activity against Botrytis cinerea, with the EC₅₀ value of 18 μg/ml, than that of Carbendazim. To the best of our knowledge, this is the first report on the antibacterial and antifungal activities of this series of novel thiochromanone derivatives containing an oxime or oxime ether moiety.

中文翻译：

含有肟或肟醚部分的新型硫代色满酮衍生物的设计、合成和生物活性评估

本研究以植物活性成分硫色满酮为先导化合物，设计合成了一系列含有肟或肟醚部分的新型硫色满酮衍生物。化合物4a对米黄单胞菌pv的半数最大有效浓度 (EC ₅₀ ) 值。米( Xoo ),米黄单胞菌pv 。oryzicolaby ( Xoc ) 和Xanthomonas axonopodis pv 。citri ( Xac ) 分别为 6、10 和 15 μg/ml，优于双美噻唑和噻二唑铜。同时，化合物4a还显示出比多菌灵更好的抗灰霉病菌的抗真菌活性，EC ₅₀值为 18 μg/ml。据我们所知，这是关于该系列含有肟或肟醚部分的新型硫代色满酮衍生物的抗菌和抗真菌活性的首次报告。

更新日期：2021-07-05

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