Pharmacological Effects of Benzimidazole Derivatives
Keywords:
Heterocycle, Benzimidazole, Pharmacological Activities, Drug DesignAbstract
In the field of Medicinal Chemistry, the uses of heterocyclic compounds increased day by day, because in many biological materials, heterocyclic compound is a part of its structure. Benzimidazole is a heterocyclic compound which formed by fusion of benzene and imidazole. Benzimidazole contains two nitrogen’s as heteroatom. Benzimidazole derivatives are more effective, medicinally useful compounds and extensive biochemicals. Derivatives of benzimidazole have found practical applications in various fields. These nitrogen-containing bicyclic structures are structural analogs of purines and have been extensively studied due to their diverse biological activities, including antifungal, antidiabetic, antiviral, anticancer, anti-inflammatory, and antimicrobial effects. This paper is summarized to know about the chemistry of different derivatives of substituted benzimidazoles along with their pharmacological activities. The molecular versatility of benzimidazole allows for functional modifications that enhance bioavailability and potency, making it a valuable scaffold in medicinal chemistry.
Downloads
References
Arora, P., Arora, V., Lamba, H. S., & Wadhwa, D. (2012). Importance of heterocyclic chemistry: A review. International Journal of Pharmaceutical Sciences and Research, 3(9), 2947.
Anand, K., & Wakode, S. (2017). Development of drugs based on benzimidazole heterocycle: recent advancement and insights. Int. J. Chem. Stud, 5(2), 350-362.
Negi, D. S., Kumar, G., Singh, M., & Singh, N. (2017). Antibacterial activity of benzimidazole derivatives: A mini review. Research & Reviews: Journal of Chemistry, 6, 18-28.
Mohammed, L. A., Farhan, M. A., Dadoosh, S. A., Alheety, M. A., Majeed, A. H., Mahmood, A. S., & Mahmoud, Z. H. (2023). A review on benzimidazole heterocyclic compounds: Synthesis and their medicinal activity applications. SynOpen, 7(04), 652-673.
Pathare, B., & Bansode, T. (2021). Biological active benzimidazole derivatives. Results in Chemistry, 3, 100200.
Ravichandiran Velayutham, V. S., & Gupta, S. (2022). Overview on Biological Activities. Nanostructured Biomaterials: Basic Structures and Applications, 135.
Patil, A., Ganguly, S., & Surana, S. (2008). A systematic review of benzimidazole derivatives as an antiulcer agent. Rasayan J. Chem, 1(3), 447-460.
Kubo K, Oda K, Kaneko T, Satoh H and Nohara A. Synthesis of 2-(4- Fluoroalkoxy-2-pyridyl) methyl] sulfinyl]-1H-benzimidazoles as Antiulcer Agents. Chem Pharm Bull. 1990;38(10):2853-2858.
He, Y., Wu, B., Yang, J., Robinson, D., Risen, L., Ranken, R., ... & Swayze, E. E. (2003). 2-Piperidin-4-yl-benzimidazoles with broad spectrum antibacterial activities. Bioorganic & medicinal chemistry letters, 13(19), 3253-3256.
Spasov, A. A., Yozhitsa, I. N., Bugaeva, L. I., & Anisimova, V. A. (1999). Benzimidazole derivatives: Spectrum of pharmacological activity and toxicological properties (a review). Pharmaceutical Chemistry Journal, 33(5), 232-243.
Singh, L. R., Avula, S. R., Raj, S., Srivastava, A., Palnati, G. R., Tripathi, C. K. M., ... & Sashidhara, K. V. (2017). Coumarin–benzimidazole hybrids as a potent antimicrobial agent: synthesis and biological elevation. The Journal of antibiotics, 70(9), 954-961.
Natarajan, R., Kumar, P., Subramani, A., Siraperuman, A., Angamuthu, P., Bhandare, R. R., & Shaik, A. B. (2024). A Critical Review on Therapeutic Potential of Benzimidazole Derivatives: A Privileged Scaffold. Medicinal Chemistry, 20(3), 311-351.
Kumar, S., Bhatt, A., & Kant, R. (2021). Biological significance of benzimidazole derivatives: A Review. Chemistry & Biology Interface, 11(6).
Alasmary, F. A., Snelling, A. M., Zain, M. E., Alafeefy, A. M., Awaad, A. S., & Karodia, N. (2015). Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents. Molecules, 20(8), 15206-15223.
Ajani, O. O., Aderohunmu, D. V., Olorunshola, S. J., Ikpo, C. O., & Olanrewaju, I. O. (2016). Facile synthesis, characterization and antimicrobial activity of 2-alkanamino benzimidazole derivatives. Oriental Journal of Chemistry, 32(1), 109.
Aslam, M. S., Naveed, S., Ahmed, A., Abbas, Z., Gull, I., & Athar, M. A. (2014). Side effects of chemotherapy in cancer patients and evaluation of patients opinion about starvation based differential chemotherapy. Journal of Cancer Therapy, 5(8), 817-822.
Bhambra, A. S., Edgar, M., Elsegood, M. R., Horsburgh, L., Kryštof, V., Lucas, P. D., ... & Zeinali, F. (2016). Novel fluorinated benzimidazole-based scaffolds and their anticancer activity in vitro. Journal of Fluorine Chemistry, 188, 99-109.
Ibba, R., Carta, A., Madeddu, S., Caria, P., Serreli, G., Piras, S., ... & Sanna, G. (2021). Inhibition of Enterovirus A71 by a Novel 2-Phenyl-Benzimidazole Derivative. Viruses, 13(1), 58.
Tamm, I., Bablanian, R., Nemes, M. M., Shunk, C. H., Robinson, F. M., & Folkers, K. (1961). Relationship Between Structure Of Benzimidazole Derivatives And Selective Virus Inhibitory Activity Inhibition Of Poliovirus Multiplication And Cytopathic Effects By 2-(Α-Hydroxybenzyl)-Benzimidazole, And Its 5-Chloro Derivative. Journal of Experimental Medicine, 113(4), 625-656.
Ahmad, G., Sohail, M., Bilal, M., Rasool, N., Qamar, M. U., Ciurea, C., ... & Misarca, C. (2024). N-Heterocycles as promising antiviral agents: a comprehensive overview. Molecules, 29(10), 2232.
Walia, R., Hedaitullah, M., Naaz, S. F., Iqbal, K., & Lamba, H. S. (2011). Benzimidazole derivatives–an overview. Int. J. Res. Pharm. Chem, 1(3), 565-74.
Sondhi, S. M., Singh, N., Kumar, A., Lozach, O., & Meijer, L. (2006). Synthesis, anti-inflammatory, analgesic and kinase (CDK-1, CDK-5 and GSK-3) inhibition activity evaluation of benzimidazole/benzoxazole derivatives and some Schiff’s bases. Bioorganic & medicinal chemistry, 14(11), 3758-3765.
Sabat, M., VanRens, J. C., Laufersweiler, M. J., Brugel, T. A., Maier, J., Golebiowski, A., ... & Janusz, M. J. (2006). The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck). Bioorganic & medicinal chemistry letters, 16(23), 5973-5977.
Sethi, R., Arora, S., Saini, D. E. E. P. I. K. A., Singh, T. G., & Jain, S. A. N. D. E. E. P. (2017). Design and Synthesis of N-(benzimidazol-1-yl Methyl)-Benzamide Derivatives Anti-inflammatory and Analgesic Agents. ACTA Pol. Pharm, 74, 1413-1425.
Nair, S. M., Beevi, J., Nj, M., Emmanuel, B. D., Dharan, S. S., & Cr, R. (2016). Insilico Design, Synthesis and In Vitro Antidiabetic and Anti-inflammatory Activities of 1, 3, 4-Thiadiazole Substituted 2-Methyl Benzimidazole Derivatives. J. Pharm. Res. Clin. Pract, 6, 27-36.
Bharadwaj, S. S., Poojary, B., Nandish, S. K. M., Kengaiah, J., Kirana, M. P., Shankar, M. K., ... & Sannaningaiah, D. (2018). Efficient synthesis and in silico studies of the benzimidazole hybrid scaffold with the quinolinyloxadiazole skeleton with potential α-glucosidase inhibitory, anticoagulant, and antiplatelet activities for type-II diabetes mellitus management and treating thrombotic disorders. ACS omega, 3(10), 12562-12574.
Rodrigues, D. C. D. N., Porto, J. C. S., dos Santos, I. L., Filho, J. I. A. B., & Ferreira, P. M. P. (2025). Repositioning anthelmintics for the treatment of inflammatory-based pathological conditions. Inflammopharmacology, 33(2), 551-571.
Sharma, S., Goel, V., Kaur, P., Gadhave, K., Garg, N., Singla, L. D., & Choudhury, D. (2023). Targeted drug delivery using beeswax-derived albendazole-oaded solid lipid nanoparticles in Haemonchus contortus, an albendazole-tolerant nematode. Experimental Parasitology, 253, 108593.
Downloads
Published
Issue
Section
License
Copyright (c) 2025 International Journal of Scientific Research in Science and Technology

This work is licensed under a Creative Commons Attribution 4.0 International License.