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N-(1,4-二取代吡唑基)-杂环酰胺类化合物的合成及抗植病真菌生物活性

作  者:
吴志兵;何雪峰;蔡桦;邝继清;薛伟
单  位:
贵州大学精细化工研究开发中心;绿色农药与生物工程国家重点实验室培育基地和教育部重点实验室
关键词:
杂环酰胺;吡唑;合成;抗植病真菌活性
摘  要:
[目的]吡唑类化合物是一类具有广泛生物活性的化合物,为了寻找到高活性的杂环酰胺类化合物,对此类化合物做进一步研究。[方法]设计合成了12个N-(1,4-取代吡唑基)-吡啶酰胺类化合物;采用生长速率法,测试了化合物对小麦赤霉病菌(Gibberella zeae)、辣椒枯萎病菌(Fusarium oxysporum)和苹果腐烂病菌(Cytosporamandshurica)的抑制活性。[结果]初步生物活性表明:目标化合物在50 mg/L质量浓度下对小麦赤霉病菌、辣椒枯萎病菌和苹果腐烂病菌有一定的抑制作用,其中化合物9j对小麦赤霉病菌的抑制率达71.0%,化合物9l对苹果腐烂病菌的抑制率达55.7%,具有进一步研究的价值。
译  名:
Synthesis and Antifungal Activity of N-(1,4-Substitued-pyrazole-yl)-heterocyclic Carboxamide Derivatives
作  者:
WU Zhi-bing,HE Xue-feng,CAI Hua,KUANG Ji-qing,XUE Wei(Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Center for Research and Development of Fine Chemicals,Guizhou University,Guiyang 550025,China)
关键词:
heterocyclic carboxamide;pyrazole;synthesis;antifungal activity
摘  要:
[Aims]Pyrazole derivates was a kind of compounds with high and broad-spectrum activity.In order to find heterocyclic carboxamide derivatives with high activity,and this kind of compounds were further studied.[Methods]A series of N-(1,4-disubstituted pyrazole-yl)-heterocyclic carboxamide derivatives were synthesized.All target compounds were bioassayed in vitro against three kinds of phytopathogenic fungi(Gibberella zeae,Fusarium oxysporum,Cytospora mandshurica).[Results]The preliminary results indicated most of the synthesized compounds possessed some antifungal activity against these three tested fungus at 50 mg/L,among which compounds 9j displayed 71.0% inhibition activities against G.zeae at 50 mg/L,and compounds 9l displayed 55.7% inhibition activities against C.mandshurica at 50 mg/L.The molecule structures of the target compounds could be optimized based on the designed compounds.

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