Discovery of a new fungicide by screening triazole sulfonylhydrazone derivatives and its downy mildew inhibition in cucumber,Journal of Heterocyclic Chemistry

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Discovery of a new fungicide by screening triazole sulfonylhydrazone derivatives and its downy mildew inhibition in cucumber
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-02-28 , DOI: 10.1002/jhet.3932
Yitao Li ₁ , Jian Lin ₁ , Wenqiang Yao ₁ , Guoliang Gao ₁ , Dewang Jing ₁ , Yang Wu ₁

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Downy mildew is a very important detrimental disease that lead reduced to fruits and vegetables. Due to the continuous growth of drug resistance, finding novel fungicides with dissimilar modes of function from present fungicides for controlling downy mildew are imminent. This work is an extension of our preceding research on the original triazole sulfonamide derivatives lead compound. Triazole sulfonamide as a remarkable nitrogen‐containing heterocyclic compound opposed cucumber downy mildew (CDM) develops a quite vital part in the sphere of the study of new farm chemicals. The existing report designs a certain amount of 1,2,4‐triazole‐1,3‐disulfonamide derivatives. Hydrazones have obtained extensive attention in the field of pharmaceutical due to its unique chemical structure and remarkable activity (insecticidal, antibacterial, antifungal and herbicidal). By means of coupling numerous hydrazone with triazole sulfonyl chloride groups, 24 novel derivatives were synthesized. Spectrum analysis of LC‐MS, ¹H NMR and ¹³C NMR were used for characterizing these new compounds. Compared with commercial Cyazofamid using bioassays, most of these compounds displayed preferable fungicidal activities. Moreover, compounds 8q illustrated the greatest CDM resistance (EC₅₀ = 7.776 mg/L). Field efficacy trials revealed that compound 8q fungicidal activity was higher than the purchased agrochemical Cyazofamid and Amisulbrom. Thus, the research declared that 8q displayed a great potential for the application of fungicide against CDM.

中文翻译：

通过筛选三唑磺酰hydr衍生物发现一种新型杀菌剂及其对黄瓜的霜霉病抑制作用

霜霉病是一种非常重要的有害疾病，可导致水果和蔬菜减少。由于耐药性的持续增长，迫切需要从目前的用于控制霜霉病的杀真菌剂中找到功能模式不同的新型杀真菌剂。这项工作是对我们先前对原始三唑磺酰胺衍生物铅化合物的研究的扩展。三唑磺酰胺是一种出色的含氮杂环化合物，可与黄瓜霜霉病（CDM）对抗，在新型农用化学品研究领域中发挥了至关重要的作用。现有报告设计了一定数量的1,2,4-三唑-1,3-二磺酰胺衍生物。dra因其独特的化学结构和出色的活性（杀虫，抗菌，抗真菌和除草剂）。通过将许多与三唑磺酰氯基团偶合，合成了24种新的衍生物。LC-MS的频谱分析¹ H NMR和¹³ C NMR用于表征这些新化合物。与使用生物测定法的商业氰唑胺相比，这些化合物大多数显示出较好的杀真菌活性。此外，化合物8q表现出最大的CDM抗性（EC ₅₀ = 7.776 mg / L）。田间功效试验表明，化合物8q的杀真菌活性高于购买的农业化学产品Cyazofamid和Amisulbrom。因此，研究表明8q展示了在CDM上使用杀真菌剂的巨大潜力。

更新日期：2020-02-28

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