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Chinese Journal of Organic Chemistry >

2023 , Vol. 43 >Issue 2: 686 - 696

DOI: https://doi.org/10.6023/cjoc202206030

Design, Synthesis and Antifungal Bioactivity Evaluation of Thiazole Benzoate Derivatives

  • Meng Li ,
  • Dongguo Xia ,
  • Yunxiao Wang ,
  • Xiang Cheng ,
  • Jiexiu Gong ,
  • Yao Chen ,
  • Xianhai Lü
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  • School of Science, Anhui Agricultural University, Hefei 230036
†(The authors contributed equally to this work).
* Corresponding author. E-mail:

Received date: 2022-06-18

  Revised date: 2022-09-04

  Online published: 2022-10-25

Supported by

Anhui Provincial Natural Science Foundation for Distinguished Young Scholars(2008085J09); National Natural Science Foundation of China(32272584)

Fold

Abstract

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

Cite this article

Meng Li , Dongguo Xia , Yunxiao Wang , Xiang Cheng , Jiexiu Gong , Yao Chen , Xianhai Lü . Design, Synthesis and Antifungal Bioactivity Evaluation of Thiazole Benzoate Derivatives[J]. Chinese Journal of Organic Chemistry, 2023 , 43(2) : 686 -696 . DOI: 10.6023/cjoc202206030

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