3,6-二苯氧甲基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑衍生物的合成及生物活性

Synthesis and Biological Activities of Derivatives of 3,6-Diphenoxymethyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles

以4-氨基-5-苯氧甲基-3-巯基-1,2,4-三唑和取代苯氧乙酸为原料,三氯氧磷为脱水剂和反应溶剂,设计合成了3,6-二苯氧甲基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑衍生物.采用IR,1HNMR和元素分析确定了各化合物的化学结构,并对其进行了室内毒力测试.生物活性结果表明,此类化合物具有较好的杀菌活性,化合物3c,3h和3f对所测试的3种植物病菌的EC50和EC95值均小于对照药剂;A和B环中有一个取代基为邻硝基时杀菌抑菌活性较好.

In order to synthesize new trizolothiadiazole derivatives and investigate the relationship between structure and biological activity,3,6-diphenoxymethyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles were designed and synthesized by 4-amino-5-（phenoxymethyl）-3-mercapto-1,2,4-triazole and substituted phenoxyacetic acid in dehydratent and solvent POCl3.The chemical structures of the compounds were confirmed by 1H NMR,IR and elemental analysis.The preliminary toxicity testing of all the target compounds were investigated.The results show that they exhibited melt fungicidal activities.The values of EC50 and EC95 of compounds 3c,3h and 3f are smaller than the comparison compound to the three pathogen.The compound which contains one 2-nitro in A or B ring has better biological activity than the others,further study is underway.