Design,Synthesis And Fungicidal Activity Of Thiazole-5-carboxamide Derivatives

As a five-membered aromatic heterocycles with distinctive structures and activity characteristics,thiazole has a wide range of applications in the fields of medicine and pesticides,such as the anticancer drug dasatinib,the antibiotic drug cefixime,the fungicide thifluzamide and etc.The design and synthesis of novel thiazolamides compounds have important theoretical and application significance for unique fungicides.In this paper,the application of thiazoles in the field of pesticides has been fully investigated.Based on the development of insecticide and the biological activity screening work of the group,the thiazolamides derivatives having a certain fungicidal activity while having insecticidal activity was selected as lead compounds.The relationship between its structure and fungicidal activity,37 thiazolamides target compounds with novel structures were designed and synthesized by molecular design of pesticides such as combination of bioactive sub-structures and bio-electronic isotope.Its structural formula is as follows.The structures of all the target compounds were confirmed by NMR 、 GC-MS and LC-MS.The fungicidal,insecticidal and herbicidal activities of this compounds were tested.The results of fungicidal activities showed that the W3 could achieve more than 90% of level-A against Phytophythora capsici and Alternaria alternata by the method of mycelial growth rate at an experimental concentration of 25 mg/L.W12,W14,W15,etc.have more than 90% of level-A fungicidal activity against Erysiphe graminis by the method of greenhouse trials at an experimental concentration of 500mg/L;the compounds of W1,W12,W24,etc.have 90% control effect against Corn Rusts;the compounds of W2,W12,W14,etc.have more than 90% A-grade control effect against Rhizoctonia solani,among which W21 and W22 have the same level with thifluzamide.The results of insecticidal activities showed that the W1 and W17 have more than 90% A-grade activity against Tetranychus urticae at an experimental concentration of 500 mg/L.Further screening results showed that the acaricidal activity of W17 against Tetranychus urticae was superior to that of the commercial insecticide spirotetramat.The relationship between structure and biological activity was summarized of the target compounds,which has important guiding significance for further research.