化学学报 ›› 2001, Vol. 59 ›› Issue (4): 594-599. 上一篇    下一篇

研究论文

5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-硫乙酰腙类 衍生物的合成及生物活性 研究

杨光富;刘祖明;陆爱红;庄农波   

  1. 华中师范大学农药研究所
  • 发布日期:2001-04-15

Syntheses and biological activity of 5,7-dimethyl- 1,2,4-triazolo[1, 5-a]pyrimidine-2-thioacetohydrazones

Yang Guangfu;Liu Zuming;Lu Aihong;Zhuang nongbo   

  • Published:2001-04-15

以2-巯基-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶为起始原料,设计合成了16种新型的-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-硫乙酰腙类衍生物,其结构均经1^HNMR,MS及元素分析确证。通过核磁共振氢谱分析及分子力学优化,对该类化合物在溶液中的顺反异构体的化学位移进行了归属。初步生测结果表明,所合成的化合物均表现出不同程度的除草及杀菌活性,尤其是在50×^-6浓度下所有化合物都对水稻纹枯病表现出很好的抑制效果。对化合物4c和4o活体小株实验结果表明,在先接菌后施药的处理方式下,化合物在50×^-6和100×^-6浓度下对水稻纹枯病的防效均优于多菌灵和井冈霉素,在100×^-6浓度下的防效达到了80%以上。

关键词: 三唑P, 嘧啶P, 腙P, 生物活性, 质子磁共振谱法, 质谱法, 化学位移, 农药, 杀菌性

Sixteen novel 5,7-dimethyl-1,2,4-triazolo[1,5-a] pyrimidine-2 thioacetohydrazone derivatives have been designed and synthesized based on the starting material 2-mercapto-5,7-dimethyl-1,2,4-triazolo [1,5-a]pyrimidine. All compounds synthesized are identified by 1^H NMR, MS and elemental analyses. Cis/trans isomers of the compounds are observed in solutions by analyzing the NMR spectroscopy and the chemical shifits of the cis/trans isomers are assigned by molecular mechanics method. Preliminary bioassay indicates that all the compounds display herbicidal activity to some extent and excellent fungicidal activity against rhizoctonia solani.

Key words: PYRRODIAZOLE P, PYRIMIDINE P, HYDRAZONE P, BIOLOGICAL ACTIVITY, PROTON MAGNETIC RESONANCE SPECTROMETRY, MASS SPECTROGRAPHY, CHEMICAL SHIFT, PESTICIDES

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