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Benzimidazole, also known as m-diazindene and benzodiazole, molecular formula C7H6N2. Benzimidazole ring is an aromatic heterocycle with two nitrogen atoms. This special structure can form hydrogen bond with enzymes and receptors in vivo, coordinate with metal ions, and generate hydrophobic hydrophobic and π - π interactions.


Benzimidazole and its derivatives are widely used in many fields, such as functional materials, pharmaceuticals, textiles, fungicides, pesticides and so on. Some of its metal complexes have bactericidal and anticancer activities, which are of great significance in the simulation of metalloenzymes.


Recent studies have shown that benzimidazole and its derivatives can be used as pharmaceutical intermediates. Due to its special structure, benzimidazole has a wide range of biological activities, such as antiviral, anticancer, antibacterial and so on. It can be used to simulate the active sites of natural superoxide dismutase (SOD), carboxyanhydrase and acid phosphatase. Benzimidazole can be used as the biological isomer of purine. Purine is very important for the biosynthesis of bacterial cell wall, nucleic acid and protein. In addition, the clinical use of benzimidazoles has the characteristics of high efficiency and low toxicity in the process of anti-bacterial and anti-inflammatory. The research shows that benzimidazoles have antibacterial effect on Gram-negative and positive bacteria. Since the research on benzimidazole and its derivatives has been more than a century, in 1955, scientists found that 5,6-dimethylbenzimidazole is a component of vitamin B12. Through this important discovery, scientists gradually found that benzimidazole and its derivatives have spectral biological activity, and benzimidazole compounds are low toxic and have strong bactericidal activity, At the same time, its special reactivity has also attracted much attention. It is also an important intermediate in many organic synthesis. Benzimidazole derivatives can also be used as metal corrosion inhibitors. The drug molecules constructed by benzimidazole ring have been used in clinical treatment for many diseases, such as astemizole and Mizolastine for allergic inflammation such as allergic rhinitis, omeprazole and rabeprazole for gastric ulcer, telmisartan and candesartan for antihypertensive, albendazole, albendazole and mebendazole for antiparasitic.


Some researchers have found that benzimidazole carbamate in benzimidazole derivatives is a very effective anti insect drug. This kind of anti insect drug develops very rapidly, and this kind of anti insect drug has a wide range of uses. It is the first choice in the treatment of many parasitic helminth diseases.

Benzimidazoles and deriviatesFig 1. Benzimidazoles and deriviates


  1. Uslu A G, Maz T G, Nocentini A, et al. Benzimidazole derivatives as potent and isoform selective tumor-associated carbonic anhydrase IX/XII inhibitors[J]. Bioorganic Chemistry, 2019: 103544.
  2. Dokla E M E, Abutaleb N S, Milik S N, et al. Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria[J]. European journal of medicinal chemistry, 2020, 186: 111850.


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