2-甲基-1-(4-芳基噻唑-2-基)-苯并咪唑-6-甲酸乙酯的合成、表征及生物活性

Synthesis,Characterization and Biological Activity of Ethyl 2-Methyl-1-(4-arylthiazol-2-yl)-benzoimidazole-6-carboxylate

以4-乙酰氨基苯甲酸乙酯为原料设计合成了14种2-甲基-1-(4-芳基噻唑-2-基)-苯并咪唑-6-甲酸乙酯新化合物.化合物结构经质谱、1H NMR、红外光谱和元素分析等确证,并用单晶X射线衍射仪测定了化合物5a的晶体结构.生物活性实验结果表明,化合物5c(500mg/L)对小麦白粉病菌抑制率达到95%;化合物5e对辣椒疫霉病菌(25mg/L)的抑制率为61.9%,对油菜菌核病菌(500mg/L)抑制率高达97.2%;化合物5k(25mg/L)对小麦赤霉病菌抑制率为55.1%.

Compounds containing thiazole or benzoimidazole ring system are found to exhibit a wide spectrum of biological activities. Fourteen new ethyl 2-methyl-i-（4-arylthiazol-2-yl）-benzoimidazole-6-carboxylates were synthesized from ethyl 4-acetamidobenzoate with four steps. Their structures were clearly established by MS, 1H NMR spectra and elemental analysis. The crystal structure of compound 5a was determined by X-ray diffraction analysis. The preliminary bioassays indicate that compound 5c exhibited 95% inhibition rate against E. graminis at 500 mg/L; compound 5e exhibited 61.9% inhibition rate against P. capsici at 25 mg/L. compound 5e exhibited 97.2% inhibition rate against S. sclerotiorum at 500 rag/L, and compound 5k exhibited 55.1% inhibition rate against G. zeae.