Design,synthesis And Activity Study Of Benzimidazoles

Benzimidazole is a heterocyclic compound with a variety of biological activities and a wide range of applications.It is widely used in many fields such as sterilization,pharmaceuticals,corrosion inhibitors and catalysts.Because the different groups can be introduced to the 1st N and the 2nd positions,it has a very wide research space and also a research hotspot.In this work,2-N-substituted benzyl benzimidazoles were synthesized by using2-aminobenzimidazole as the backbone.A synthetic route was designed based on this type of compound,and finally 12 benzimidazole derivatives were synthesized,of which 5 were not reported in the literature.The target compounds were characterized by ~1H NMR and MS,and their stuctures were confirmed.We were tested the preliminarily antimicrobial activity of 12 compounds by mycelial growth rate method,and the antimicrobial activity was not reported in the literature.The tested strains were Fusarium graminearum,Fusarium graminearum Mutation 200,Fusarium graminearum Mutation 198 and Botrytis cinerea.At a concentration of 50?g/m L.Among the 12 compounds,the inhibition rate of D1k against Fusarium graminearum was67%,and the inhibition rate of compound D1k against Fusarium graminearum(Mutation200)was 69%,the inhibition rate of compound D1e against Fusarium graminearum(Mutation 198)was 75%,and the inhibition rate of compound D1i against Botrytis cinerea was 60%.By analyzing the inhibition rate of the these compounds,the compound which has two meta-chlorine substitutes in the aromatic rings showed high antimicrobial activity,this compound has potential for further research.