新型吡唑-4-酰胺类衍生物设计、合成与生物活性

为寻找高生物活性的吡唑酰胺类化合物,设计、合成一系列含硫结构的N-吡啶基吡唑-4-酰胺类衍生物,目标化合物结构经1HNMR、13CNMR和有机元素分析或高分辨质谱确证,并进行了杀虫及杀菌活性测试研究。初步杀虫活性测试结果表明,目标化合物在200mg/L对东方粘虫具有中等杀虫活性。同时,测试了目标化合物在50mg/L对5种病菌的离体抑菌活性,化合物N-(4-氯-2-甲基-6-甲酰胺基)苯基]-1-(3-氯-2-吡啶基)-3-硫甲基-1H-吡唑-4-甲酰胺If和N-(4-氯-2-甲基-6-环丙基酰胺基)苯基]-1-(3-氯-2-吡啶基)-3-硫甲基-1H-吡唑-4-甲酰胺Ig对番茄早疫病菌显示了良好的活性,分别为65.2%和67.1%, 高于对照药百菌清,值得进一步研究。

Synthesis and Biological Evaluation of Novel N-pyridylpyrazole-4-carboxamides Containing Sulfur Moiety

To develop new compounds with high biological activity, a series of novel N-pyridylpyrazole-4-carboxamides containing sulfur moiety were designed and synthesized. The target compounds were identified by 1H NMR, 13C NMR, high-resolution mass spectrum (HRMS) or elemental analysis. The insecticidal activities of new compounds against oriental armyworm (Mythimna separata) were evaluated. The results of bioassays indicated that the title compounds showed moderate activities at the 200mg/L. Moreover, the fungicidal activities in vitro against five fungi at 50 mg/L indicated that some compounds exhibited promising fungicidal activities. Especially, N-4-chloro-2-methyl-6-(methylcarbamoyl)phenyl]-1-(3-chloropyridin -2-yl)-3- (methylsulfanyl)-1H-pyrazole-4-carboxamide If and N-4-chloro-2-(cyclopropylcarbamoyl)-6-methylphenyl] -1-(3-chloropyridin-2-yl)-3-(methylsulfanyl)-1H-pyrazole-4-carboxamide Ig displayed a good fungicidal activity against Alternaria solani, the inhibitory rate were 65.2% and 67.1%, respectively, which was higher than the positive control compound chlorothalonil.