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Design, Synthesis, and Fungicidal Evaluation of Novel N-Methoxy Pyrazole-4-Carboxamides as Potent Succinate Dehydrogenase Inhibitors
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2023-01-25 , DOI: 10.1021/acs.jafc.2c07031 Hua Li 1, 2 , Zheng Liu 2 , Ying Dong 2 , Yu-Xia Wang 2 , Xiao-Lei Zhu 2
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2023-01-25 , DOI: 10.1021/acs.jafc.2c07031 Hua Li 1, 2 , Zheng Liu 2 , Ying Dong 2 , Yu-Xia Wang 2 , Xiao-Lei Zhu 2
Affiliation
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Succinate dehydrogenase (SDH, EC 1.3.5.1, also known as complex II) has been recognized as one of the most promising targets of fungicides. Here, based on the binding mode of pydiflumetofen with SDH, the carbon–carbon double bond was introduced into the chemical of pydiflumetofen and then produced the target compounds 6a–6o. The enzymatic inhibitory activity and structure–activity relationship (SAR) study showed that the 2-position and 4-position in terminal benzene were positive to increasing activity. Furthermore, fungicidal activity results in greenhouses indicated that compound 6o showed good control effects against wheat powdery mildew (WPM), cucumber powdery mildew (CPM), and southern corn rust (SCR), showing its broad-spectrum property. Especially, compound 6o exhibited 95 and 75% control effects against CPM and SCR at 6.25 mg/L, respectively, which are better than pydiflumetofen (80% control effects against CPM and 15% against SCR), indicating its potency that is worthy of further development.
中文翻译：
新型 N-甲氧基吡唑-4-甲酰胺作为强效琥珀酸脱氢酶抑制剂的设计、合成和杀菌评价
琥珀酸脱氢酶（SDH，EC 1.3.5.1，又称复合物II）已被公认为最有希望的杀菌剂靶点之一。在这里，基于吡草醚与SDH的结合方式，将碳-碳双键引入吡草醚的化学物质中，然后生成目标化合物6a - 6o。酶促抑制活性和结构-活性关系（SAR）研究表明，末端苯的2位和4位对活性增加呈正向。此外，温室中的杀真菌活性结果表明化合物6o对小麦白粉病（WPM）、黄瓜白粉病（CPM）和南方玉米锈病（SCR）均有较好的防治效果，显示出其广谱性。特别是，化合物6o在 6.25 mg/L 时对 CPM 和 SCR 的防治效果分别为 95% 和 75%，优于吡氟草胺（对 CPM 的防治效果为 80%，对 SCR 的防治效果为 15%），表明其效力值得进一步研究发展。
更新日期：2023-01-25
中文翻译：
新型 N-甲氧基吡唑-4-甲酰胺作为强效琥珀酸脱氢酶抑制剂的设计、合成和杀菌评价
琥珀酸脱氢酶（SDH，EC 1.3.5.1，又称复合物II）已被公认为最有希望的杀菌剂靶点之一。在这里，基于吡草醚与SDH的结合方式，将碳-碳双键引入吡草醚的化学物质中，然后生成目标化合物6a - 6o。酶促抑制活性和结构-活性关系（SAR）研究表明，末端苯的2位和4位对活性增加呈正向。此外，温室中的杀真菌活性结果表明化合物6o对小麦白粉病（WPM）、黄瓜白粉病（CPM）和南方玉米锈病（SCR）均有较好的防治效果，显示出其广谱性。特别是，化合物6o在 6.25 mg/L 时对 CPM 和 SCR 的防治效果分别为 95% 和 75%，优于吡氟草胺（对 CPM 的防治效果为 80%，对 SCR 的防治效果为 15%），表明其效力值得进一步研究发展。
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