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

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

研究论文

苯甲酸噻唑酯类衍生物的设计、合成及抗真菌活性评价

  • 李猛 ,
  • 夏东国 ,
  • 王云霄 ,
  • 程祥 ,
  • 巩杰秀 ,
  • 陈耀 ,
  • 吕献海
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  • 安徽农业大学理学院 合肥 230036
†共同第一作者

收稿日期: 2022-06-18

  修回日期: 2022-09-04

  网络出版日期: 2022-10-25

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)

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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)

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摘要

植物病原真菌严重威胁作物安全, 迫切需要开发新型高效低毒的杀菌剂. 因此, 设计、合成了一系列新型苯甲酸噻唑酯衍生物. 体外抗真菌活性筛选结果表明, 化合物3、5和8对灰霉病菌和核盘病菌均表现出良好的抗真菌活性. 其中化合物8对灰霉病菌和核盘病菌的EC50值分别为13.82和3.66 mg/L. 初步的生理生化实验结果表明化合物8对菌丝细胞膜造成一定程度的损伤.

关键词： 苯甲酸; 噻唑; 抗真菌活性; 核盘病菌; 灰霉病菌

本文引用格式

李猛 , 夏东国 , 王云霄 , 程祥 , 巩杰秀 , 陈耀 , 吕献海 . 苯甲酸噻唑酯类衍生物的设计、合成及抗真菌活性评价[J]. 有机化学, 2023 , 43(2) : 686 -696 . DOI: 10.6023/cjoc202206030

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

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