Chinese Journal of Organic Chemistry ›› 2023, Vol. 43 ›› Issue (2): 686-696.DOI: 10.6023/cjoc202206030 Previous Articles     Next Articles


李猛, 夏东国, 王云霄, 程祥, 巩杰秀, 陈耀, 吕献海*()   

  1. 安徽农业大学理学院 合肥 230036
  • 收稿日期:2022-06-18 修回日期:2022-09-04 发布日期:2022-10-24
  • 作者简介:
  • 基金资助:
    安徽省杰出青年科学基金(2008085J09); 国家自然科学基金(32272584)

Design, Synthesis and Antifungal Bioactivity Evaluation of Thiazole Benzoate Derivatives

Meng Li, Dongguo Xia, Yunxiao Wang, Xiang Cheng, Jiexiu Gong, Yao Chen, Xianhai Lü()   

  1. School of Science, Anhui Agricultural University, Hefei 230036
  • Received:2022-06-18 Revised:2022-09-04 Published:2022-10-24
  • Contact: *E-mail:
  • About author:
    †(The authors contributed equally to this work).
  • Supported by:
    Anhui Provincial Natural Science Foundation for Distinguished Young Scholars(2008085J09); National Natural Science Foundation of China(32272584)

Plant pathogenic fungi seriously threaten agricultural production, and there is an urgent need to develop new high efficiency and low toxicity fungicides. In this article, a series of new thiazole benzoate derivatives are designed and synthesized. The preliminary screening results showed that 1-(4,5-dimethylthiazol-2-yl)-2-methylpropyl benzoate (3), (3- chlorophenyl)(4,5-dimethylthiazol-2-yl)methyl benzoate (5), and (4,5-dimethylthiazol-2-yl)(m-tolyl)methyl benzoate (8) showed good inhibitory activities against Botrytis cinerea and Sclerotinia sclerotiorum. Among them, compound 8 has the best inhibitory activity against Botrytis cinerea and Sclerotinia sclerotiorum with EC50 values of 13.82 and 3.66 mg/L, respectively. Preliminary physiological and biochemical experiments showed that compound 8 caused certain damage to Sclerotinia sclerotiorum cell membrane.

Key words: benzoicacid, thiazole, antifungal activity, Sclerotinia sclerotiorum, Botrytis cinerea