新型含砜基腙部分的噻吩并[2,3-b]吡啶酮衍生物的设计、合成与生物活性评价。
Novel Thiochromanone Derivatives Containing a Sulfonyl Hydrazone Moiety: Design, Synthesis, and Bioactivity Evaluation.
机构信息
School of Liquor and Food Engineering, Guizhou University, Guiyang 550025, China.
Qiandongnan Engineering and Technology Research Center for Comprehensive Utilization of National Medicine, Kaili University, Kaili 556011, China.
出版信息
Molecules. 2021 May 14;26(10):2925. doi: 10.3390/molecules26102925.
A series of novel thiochromanone derivatives containing a sulfonyl hydrazone moiety were designed and synthesized. Their structures were determined by H-NMR, C-NMR, and HRMS. Bioassay results showed that most of the target compounds revealed moderate to good antibacterial activities against pv. , pv. , and pv. . Compound had the best inhibitory activity against pv. , pv. , and pv. , with the EC values of 8.67, 12.65, and 10.62 μg/mL, which were superior to those of Bismerthiazol and Thiodiazole-copper. Meanwhile, bioassay results showed that all of the target compounds proved to have lower antifungal activities against , , , , , and than those of Carbendazim.
设计并合成了一系列含有磺酰腙部分的新型噻吩并[2,3-b]吡啶酮衍生物。它们的结构通过 H-NMR、C-NMR 和 HRMS 确定。生物测定结果表明，大多数目标化合物对 pv. 、 pv. 、 pv. 具有中等至良好的抗菌活性。化合物 对 pv. 、 pv. 、 pv. 的抑制活性最好，EC 值分别为 8.67、12.65 和 10.62 μg/mL，优于双甲脒和噻二唑铜。同时，生物测定结果表明，所有目标化合物对 、 、 、 、 和 的抑菌活性均低于多菌灵。
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