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  

Synthesis and Antifungal Activity of N-(1,4-Substitued-pyrazole-yl)-heterocyclic Carboxamide Derivatives

作　　者：吴志兵[1] 何雪峰[1] 蔡桦[1] 邝继清[1] 薛伟[1] 

机构地区：[1]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,贵阳550025

出　　处：《农药》2013年第1期11-14,44,共5页Agrochemicals

基　　金：贵州省自然科学研究项目(2010008);贵州省科学技术基金(20112064);国家自然科学基金(21062005)

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。[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 91 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.

关 键 词：杂环酰胺 吡唑 合成 抗植病真菌活性 

分 类 号：TQ450.2[化学工程—农药化工]