Synthesis and Fungicidal Activities of New 1,2,4-Triazolo[1,5-a]pyrimidines
Synthesis and Fungicidal Activities of New 1,2,4-Triazolo[1,5-a]pyrimidines
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新型1,2,4-三唑并[1,5-a]嘧啶类化合物的合成及其杀菌活性
DOI：
10.1002/cbdv.200800168
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发表时间：
2009-01-01
影响因子：
2.9
通讯作者：
Yang, Guang-Fu
中科院分区：
文献类型：
--
作者：
Chen, Qiong;Liu, Zu-Ming;Yang, Guang-Fu
为寻找具有较高杀菌活性的新型农药，设计合成了一系列含乙酰腙的1，2，4-三唑并[1，5-a]嘧啶衍生物。对它们进行了离体抑菌活性评价，筛选出最有前途的化合物2-[（5，7-二甲基[1，2，4]三唑并[1，5-a]嘧啶-2-基）硫烷基]-2 '-[（2-羟基苯基）亚甲基]乙酰肼（2-17），结果表明，其EC 50值（5.34 μ g ml（-1））低于市售多菌灵（EC 50 = 7.62 μ g ml（-1））。此外，化合物2-17还显示出广谱杀菌活性，其对灰葡萄孢的EC_（50）值（4.56 μ g·ml ~（-1））与多菌灵非常相似。并对所合成化合物的构效关系进行了讨论。
A series of new acetohydrazone-containing 1,2,4-triazolo[1,5-a]pyrimidine derivatives were designed and synthesized for the purpose of searching for novel agrochemicals with higher fungicidal activity. Their in vitro fungicidal activities against Rhizoctonia solani were evaluated, and the most promising compound, 2-[(5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfanyl]-2'-[(2-hydroxyphenyl)methylidene]acetohydrazide (2-17), showed a lower EC50 value (5.34 mu g ml(-1)) than that of commercial carbendazim (EC50 = 7.62 mu g ml(-1)). Additionally, compound 2-17 was also found to display broadspectrum fungicidal activities, and its EC50 value (4.56 mu g ml(-1)) against Botrytis cinereapers was very similar to that of carbendazim. Qualitative structure-activity relationships (QSARs) of the synthesized compounds were also discussed.