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高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (5): 781-785.doi: 10.1007/s40242-016-6153-z

• Articles • 上一篇    下一篇

Syntheses and Fungicidal Activities of Thiazole-5-carboxanilides Bearing Thioether Group

XUE Hansong1,2, LIU Aiping2,3, LIU Weidong2,3, LI Jianming2, REN Yeguo2, HUANG Lu2,3, HE Lian2, OU Xiaoming2, YE Jiao1, HUANG Mingzhi2,4   

  1. 1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P. R. China;
    2. National Engineering Research Center for Agrochemicals, Hunan Research Institute of Chemical Industry, Changsha 410007, P. R. China;
    3. Hunan Province Key Laboratory for Agrochemicals, Hunan Research Institute of Chemical Industry, Changsha 410014, P. R. China;
    4. Hunan Haili Chemical Industry Co., Ltd., Changsha 410007, P. R. China
  • 收稿日期:2016-04-22 修回日期:2016-05-30 出版日期:2016-10-01 发布日期:2016-09-24
  • 通讯作者: YE Jiao, HUANG Mingzhi E-mail:yejiao@hnu.edu.cn;huang-mz@163.com
  • 基金资助:

    Supported by the National Natural Science Foundation of China(Nos.21272062, 21572050).

Syntheses and Fungicidal Activities of Thiazole-5-carboxanilides Bearing Thioether Group

XUE Hansong1,2, LIU Aiping2,3, LIU Weidong2,3, LI Jianming2, REN Yeguo2, HUANG Lu2,3, HE Lian2, OU Xiaoming2, YE Jiao1, HUANG Mingzhi2,4   

  1. 1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P. R. China;
    2. National Engineering Research Center for Agrochemicals, Hunan Research Institute of Chemical Industry, Changsha 410007, P. R. China;
    3. Hunan Province Key Laboratory for Agrochemicals, Hunan Research Institute of Chemical Industry, Changsha 410014, P. R. China;
    4. Hunan Haili Chemical Industry Co., Ltd., Changsha 410007, P. R. China
  • Received:2016-04-22 Revised:2016-05-30 Online:2016-10-01 Published:2016-09-24
  • Contact: YE Jiao, HUANG Mingzhi E-mail:yejiao@hnu.edu.cn;huang-mz@163.com
  • Supported by:

    Supported by the National Natural Science Foundation of China(Nos.21272062, 21572050).

摘要：

In an attempt to find leading thiazole carboxanilides exhibiting fungicidal activities, we designed and synthesized a new series of 2-sulfursubstituted thiazole carboxanilides via the reaction between 2-sulfur substituted thiazole carboxylic acid chlorides and substituted aniline. The fungicidal activities of the title compounds against Rhizoctonia solani were screened and the results were remarkable. The most potent compound 8i, N-[2,6-dichloro-4-(trifluoromethyl)phenyl]-2-methylthio-4-(trifluoromethyl)thiazole-5-carboxamide, was identified. The fungicidal EC50 of compound 8i against Rhizoctonia solani was 1.28 mg/L, being comparable to that of Thifluzamide. The results indicate that compound 8i can be considered as a lead compound for further research.

关键词: Thiazole-5-carboxamide, Fungicide, Structure-activity relationship

Abstract:

In an attempt to find leading thiazole carboxanilides exhibiting fungicidal activities, we designed and synthesized a new series of 2-sulfursubstituted thiazole carboxanilides via the reaction between 2-sulfur substituted thiazole carboxylic acid chlorides and substituted aniline. The fungicidal activities of the title compounds against Rhizoctonia solani were screened and the results were remarkable. The most potent compound 8i, N-[2,6-dichloro-4-(trifluoromethyl)phenyl]-2-methylthio-4-(trifluoromethyl)thiazole-5-carboxamide, was identified. The fungicidal EC50 of compound 8i against Rhizoctonia solani was 1.28 mg/L, being comparable to that of Thifluzamide. The results indicate that compound 8i can be considered as a lead compound for further research.

Key words: Thiazole-5-carboxamide, Fungicide, Structure-activity relationship