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

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(500 mg/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(25 mg/L)的抑制率为61.9%, 对油菜菌核病菌(500 mg/L) 抑制率高达97.2%; 化合物5k(25 mg/L) 对小麦赤霉病菌抑制率为55.1%.

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

Compounds containing thiazole or benzoimidazole ring system are found to exhibit a wide spectrum of biological activities.Fourteen new ethyl 2-methyl-1-(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 mg/L,and compound 5k exhibited 55.1% inhibition rate against G.zeae.