含3,4-二氯异噻唑并香豆素的甲氧基丙烯酸酯类杀菌剂的设计、合成及杀菌活性
Design, synthesis and fungicidal activity of 3,4-dichloroisothiazolocoumarin-containing strobilurins.
作者信息
Lv You, Li Kun, Gao Wei, Hao Zesheng, Wang Weibo, Liu Xiaoyu, Tang Liangfu, Fan Zhijin
机构信息
State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, No. 94, Weijin Road, Nankai District, Tianjin, 300071, People's Republic of China.
出版信息
Mol Divers. 2022 Apr;26(2):951-961. doi: 10.1007/s11030-021-10207-5. Epub 2021 Mar 29.
Twenty-one novel 3,4-dichloroisothiazolocoumarin-containing strobilurins were rationally designed and synthesized. Preliminary bioassay showed that compounds 7c, 7h and 7l exhibited over 80% inhibitory rate against Sclerotinia sclerotiorum at 50 μg/mL, 7c exhibited good activity against S. sclerotiorum with median effective concentration (EC) of 4.08 μg/mL, while the positive control coumoxystrobin showed EC of 1.00 μg/mL. In addition, 7d showed better fungicidal activity with a lower EC value of 7.65 μg/mL against Botrytis cinerea than that of positive control trifloxystrobin with its EC value of 21.96 μg/mL. This study indicated that 3,4-dichloroisothiazolocoumarin-containing strobilurin was a promising fungicide lead deserved for further study.
合理设计并合成了21种含3,4-二氯异噻唑并香豆素的新型甲氧基丙烯酸酯类杀菌剂。初步生物活性测试表明，化合物7c、7h和7l在50μg/mL浓度下对核盘菌的抑制率超过80%，7c对核盘菌表现出良好活性，其半数有效浓度（EC）为4.08μg/mL，而阳性对照嘧菌酯的EC值为1.00μg/mL。此外，7d对灰葡萄孢表现出较好的杀菌活性，其EC值为7.65μg/mL，优于阳性对照肟菌酯，后者的EC值为21.96μg/mL。该研究表明，含3,4-二氯异噻唑并香豆素的甲氧基丙烯酸酯类化合物是一种有潜力的杀菌剂先导化合物，值得进一步研究。
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