数字农科院2.0

Synthesis and Biological Activity of Novel Furan/Thiophene and Piperazine-Containing (Bis)1,2,4-triazole Mannich Bases

文献类型： 外文期刊

作者： Wang, Baolei;Zhan, Yizhou;Zhang, Liyuan;Zhang, Yan;Wang, Lizhong;Zhang, Xiao;Li, Yonghong;Li, Zhengming;Shi, Yanxia;Li, Baoju

作者机构：

关键词： 1,2,4-triazole;Mannich base;piperazine derivative;biological activity

期刊名称： CHINESE JOURNAL OF CHEMISTRY

ISSN： 1001-604X

年卷期： 2015 年 33 卷 10 期

页码：

收录情况： SCI

摘要： Series of novel furan/thiophene and piperazine-containing 1,2,4-triazole Mannich bases and bis(1,2,4-triazole) Mannich bases have been conveniently synthesized via Mannich reaction with triazole Schiff bases, various piperazine derivatives, and formaldehyde as intermediates in good yields. Their structures were characterized by melting points, H-1 NMR, C-13 NMR, IR and elemental analysis. The preliminary bioassay showed that most compounds exhibited significant in vitro and in vivo fungicidal activity against several test plant fungi. Among 32 new compounds, the trifluoromethyl-containing compounds showed superior activity than the methyl-containing ones. Several compounds, such as F8, F9, F10, G5, H7, H8, I3 and I4, were comparable with some commercial fungicides against different fungi during the present study and could be further structurally optimized. Meanwhile, several compounds showed good herbicidal activity against Brassica campestris at 100 mu g/mL and KARI inhibitory activity at 200 mu g/mL. However, compounds exhibited poor insecticidal activity against oriental armyworm at 200 mu g/mL in the preliminary studies. The research results will provide useful information for the design and discovery of new agrochemicals with novel heterocyclic structures.

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