2-氨基苯并咪唑衍生物的合成及抑菌活性初步研究

Synthesis and antifungal activity of 2-aminobenzimidazole derivatives

为开发新型安全、高效的杀菌剂,基于文献,设计、合成了一类2-氨基苯并咪唑衍生物。以2-氨基苯并咪唑为起始原料与不同取代的芳醛反应生成N-(^(1)H-苯并[d]咪唑-2-基)-1-取代苯基甲亚胺,然后经硼氢化钠还原得到12个目标产物。所有目标化合物经1H NMR及MS表征确证。采用菌落直径法初步测定了12个目标化合物对灰霉病病原菌的抑菌率,发现所有目标化合物在50μg/mL剂量下具有30%~60%的抑菌活性,其研究结果对开发新型杀菌剂具有一定的参考价值。

In order to develop safe and efficient fungicides,2-aminobenzimidazole derivatives were designed and synthesized based on the related literatures.2-aminobenzimidazole was used as a starting material to react with substituted aromatic aldehydes to get N-(^(1)H-benzo[d]imidazol-2-yl)-1-substituted phenylmethanimines which were reduced by sodium borohydride to obtain 12 target products.All compounds were characterized by[1H]NMR and MS.The inhibitory activity of 12 target compounds against Botrytis cinerea were investigated by the colony diameter method.It was found that all target compounds have 30%-60%inhibitory activity at 50μg/mL.The results may be to provide a reference for the development of new fungicides.