Synthesis of 1,2,3-Thiadiazole and Thiazole-Based Strobilurins as Potent Fungicide Candidates

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• 作者：Lai ChenYu-Jie Zhu ; Zhi-Jin Fan ; Xiao-Feng GuoZhi-Ming Zhang ; Jing-Hua Xu ; Ying-Qi Song ; Morzherin Y. Yurievich ; Nataliya P. Belskaya ; Vasiliy A. Bakulev
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2017
• 出版时间：February 1, 2017
• 年：2017
• 卷：65
• 期：4
• 页码：745-751
• 全文大小：390K
• ISSN：1520-5118

文摘

Strobilurin fungicides play a crucial role in protecting plants against different pathogens and securing food supplies. A series of 1,2,3-thiadiazole and thiazole-based strobilurins were rationally designed, synthesized, characterized, and tested against various fungi. Introduction of 1,2,3-thiadiazole greatly improved the fungicidal activity of the target molecules. Compounds 8a, 8c, 8d, and 10i exhibited a relatively broad spectrum of fungicidal activity. Compound 8a showed excellent activities against Gibberella zeae, Sclerotinia sclerotiorum, and Rhizoctonia cerealis with median effective concentrations (EC₅₀) of 2.68, 0.44, and 0.01 μg/mL, respectively; it was much more active than positive controls enestroburin, kresoxim-methyl, and azoxystrobin with EC₅₀ between 0.06 and 15.12 μg/mL. Comparable or better fungicidal efficacy of compound 8a compared with azoxystrobin and trifloxystrobin against Sphaerotheca fuliginea and Pseudoperonspera cubensis was validated in cucumber fields at the same application dosages. Therefore, compound 8a is a promising fungicidal candidate worthy of further development.