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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 被引量:6

Synthesis and Antifungal Activity of N-(1,4-Substitued-pyrazole-yl)-heterocyclic Carboxamide Derivatives
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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.
出处 《农药》 CAS CSCD 北大核心 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)
关键词 杂环酰胺 吡唑 合成 抗植病真菌活性 heterocyclic carboxamide pyrazole synthesis antifungal activity
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