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Novel Thiochromanone Derivatives Containing a Sulfonyl Hydrazone Moiety: Design,Synthesis, and Bioactivity Evaluation
Authors:Lu Yu  Jiyan Chi  Lingling Xiao  Jie Li  Zhangfei Tang  Shuming Tan  Pei Li
Institution:1.School of Liquor and Food Engineering, Guizhou University, Guiyang 550025, China; (L.Y.); (J.C.); (L.X.); (J.L.); (Z.T.);2.Qiandongnan Engineering and Technology Research Center for Comprehensive Utilization of National Medicine, Kaili University, Kaili 556011, China
Abstract:A series of novel thiochromanone derivatives containing a sulfonyl hydrazone moiety were designed and synthesized. Their structures were determined by 1H-NMR, 13C-NMR, and HRMS. Bioassay results showed that most of the target compounds revealed moderate to good antibacterial activities against Xanthomonas oryzae pv. oryzae, Xanthomonas oryzae pv. oryzicolaby, and Xanthomonas axonopodis pv. citri. Compound 4i had the best inhibitory activity against Xanthomonas oryzae pv. oryzae, Xanthomonas oryzae pv. oryzicolaby, and Xanthomonas axonopodis pv. citri, with the EC50 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 Sclerotinia sclerotiorum, Fusarium oxysporum, Gibberella zeae, Rhizoctonia solani, Verticillium dahlia, and Botrytis cinerea than those of Carbendazim.
Keywords:thiochromanone  sulfonyl hydrazone  antibacterial activity  antifungal activity
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