【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(Gibberellazeae)、辣椒枯萎病菌(Fusariumoxysporum)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50mg/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93对小麦赤霉病菌的抑制率达71.0%,化合物91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.