Design,Synthesis And Anti-microbial Evaluation Of Novel Benzimidazol-2-one Derivatives

Infection disease is serious threats to human health and lives.The number of deaths died of pathogenic bacteria is also growing all the time every year,so it is extremely urgent to conquer pathogenic bacteria.Nowadays,although many antibacterial drugs are using in clinical,most of them existing some problems,such as curative effect is not good enough,side effects and drug resistance and so on.Therefore,exploring the new antibacterial drugs becomes the focus of current research.benzimidazol-2-one derivatives are widely used in the field of dyes and medicine,especially in the field of medicine.The core structure of benzimidazol-2-one is a very important pharmacophore in many bioactive compounds,benzimidazol-2-one derivatives are synthesized base on the core structure has many pharmacological activities,they are widely used as antibacterial agent,antihypertensive drugs,anti-tumor agent,dopamine receptor agonists,HIV-1 non-nucleoside reverse transcriptase inhibitors,analgesic,etc.so benzimidazol-2-one derivatives have a broad application prospect.Although these compounds have many biological activities,its' antibacterial activity are rarely reported.Therefore,we modify the benzimidazole ring,designed and synthesized 15 benzimidazol-2-one derivatives and preliminary antibacterial activity was carried out in vitro.The series of compounds were synthesized starting from o-nitroaniline through a reaction sequence including N-benzylation,chlorosulfonation,substitution reduction,cyclization.The target compounds were obtained through five steps,the reagents are very common in laboratory.The synthesis condition is simpler and the experimental post-processing is also very convenient.The chemical structures of those target compounds were synthesized and confirmed by 13C NMR,IH NMR and HRMS spectral analysis.Antibacteral activity in vitro against Hemolytic streptococcus,Staphylococcus aureus,Klebsiella pneumonia and Escherichia coli were investigated by Filter paper method.Minimal inhibitory concentration(MIC)was tested by the micro dilution method.The results indicated that compound 5b has a strong inhibitory effect against Hemolytic streptococcus,MIC is 0.3125mg/ml.It also has certain antibacterial activity on Staphylococcus aureus and Escherichia coli.5g has the obvious inhibitory action against Staphylococcus aureus.It also has certain antibacterial activity on Klebsiella pneumonia.In conclusion,the series of novel benzimidazol-2-one derivatives were designed and synthesized.Preliminary antibacterial activity assay results showed that some of these compounds have potential inhibitory activity.They are a kind of potential lead compounds with great development value,and they also have very important sense for exploring a new generation of targeted antibacterial drugs...