Design, synthesis and antifungal evaluation of novel pyrazole carboxamides with diarylamines scaffold as potent succinate dehydrogenase inhibitors
作者:Aigui Zhang、Jingya Zhou、Ke Tao、Taiping Hou、Hong Jin
DOI:10.1016/j.bmcl.2018.08.001
日期:2018.10
detail via 1H NMR, 13C NMR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good antifungal activity against Rhizoctonia solani, Fusarium oxysporum, Phytophthora infestans and Fusarium graminearum. Among them, compound 1c exhibited the highest antifungal activities against R. solani in vitro with EC50 value of 0.005 mg/L, superior to the commercially available fungicide
通过1 H NMR,13 C NMR和ESI-HRMS详细设计,合成和表征了16种带有二芳基胺骨架的新型吡唑羧酰胺。初步的生物分析结果表明,一些目标化合物对茄枯萎病菌,尖孢镰刀菌,疫疫霉和禾谷镰刀菌均表现出良好的抗真菌活性。其中,化合物1c表现出最高的体外抗sol。solani真菌活性,EC 50值为0.005 mg / L,优于市售的杀菌剂fluxapyroxad(EC 50 = 0.033 mg / L)。和化合物1c(IC 50 = 0.034 mg / L)显示出对琥珀酸脱氢酶的抑制能力高于fluxapyroxad(IC 50 = 0.037 mg / L)。这项研究表明,化合物1c可被视为潜在的琥珀酸脱氢酶抑制剂。