Author(s):
Saddam Hussain, Ekta Khare, Dinesh Chandra
Email(s):
ektakhare23@gmail.com
DOI:
10.52711/0974-360X.2026.00401 
Address:
Saddam Hussain, Ekta Khare*, Dinesh Chandra
Department of Pharmaceutical Chemistry, GCRG College of Pharmacy, Lucknow, U.P., India.
*Corresponding Author
Published In:
Volume - 19,
Issue - 6,
Year - 2026
ABSTRACT:
This study presents the successful synthesis of five novel benzimidazole derivatives (S1-S5) through a meticulous, two-step synthetic route. The process commenced with the cyclization of o-phenylenediamine, followed by nucleophilic substitution reactions using various substituted anilines, strategically chosen to yield structurally diverse products. These derivatives were thoroughly characterized via advanced spectroscopic techniques, including LC-MS, 1H-NMR, and FT-IR, affirming their structural integrity and confirming the targeted framework. Antimicrobial assays showcased the promising bioactivity of S3, which exhibited noteworthy antibacterial properties against S. aureus and E. coli, with pronounced inhibition zones, attesting to their potential as antibacterial agents. Furthermore, these derivatives demonstrated potent antifungal activity, particularly against Candida albicans, underscoring their broad-spectrum antimicrobial efficacy. A significant aspect of the findings is the impact of EDGs and EWGs on the aniline moiety, which appeared pivotal in modulating the bioactivity of the synthesized compounds.
Cite this article:
Saddam Hussain, Ekta Khare, Dinesh Chandra. Exploring the Antibacterial and Antifungal potential of Benzimidazole-based Heterocycles: Synthesis, Characterization and Biological screening. Research Journal Pharmacy and Technology. 2026;19(6):2804-8. doi: 10.52711/0974-360X.2026.00401
Cite(Electronic):
Saddam Hussain, Ekta Khare, Dinesh Chandra. Exploring the Antibacterial and Antifungal potential of Benzimidazole-based Heterocycles: Synthesis, Characterization and Biological screening. Research Journal Pharmacy and Technology. 2026;19(6):2804-8. doi: 10.52711/0974-360X.2026.00401 Available on: https://rjptonline.org/AbstractView.aspx?PID=2026-19-6-58
7. REFERENCE:
1. Wright JB. The Chemistry of the Benzimidazoles. Chem Rev. 1951; 48(3): 397-541.
2. Keri, R. S., Hiremathad, A., Budagumpi, S., and Nagaraja, B. M. Comprehensive review in current developments of benzimidazole-based medicinal chemistry. Chem Biol Drug Des. 2015; 86(1): 19–65.
3. Srestha, N., Banerjee, J., and Srivastava, S. A review on chemistry and biological significance of benzimidazole nucleus. IOSRPHR. 2014; 4(12): 28–41.
4. Salahuddin, Shaharyar, M., and Mazumder, A. Benzimidazoles: A biologically active compound. Arabian Journal of Chemistry. 2017; 10: 157–173.
5. Narasimhan, B., Sharma, D., and Kumar, P. Benzimidazole: A medicinally important heterocyclic moiety. Med Chem Res. 2012; 21(3): 269–283.
6. Bansal, Y., and Silakari, O. The Therapeutic Journey of Benzimidazoles: A review. Bioorganic and Medicinal Chemistry. 2012; 20(21): 6208–6236.
7. Banerjee, S., et al. A critical review of benzimidazole: Sky-high objectives towards the lead molecule to predict the future in medicinal chemistry.Results in Chemistry. 2023; 6: 101013.
8. Prasad, P. M. K., K. A. K., and S. R. S. Potent biological agent benzimidazole–a review. Int J Pharm Sci. 2016; 8(12): 22.
9. Aonofriesei, F. Antibacterial and antifungal activity of some 2- and 1,2-substituted benzimidazole derivatives. FARMACIA. 2022; 70(3): 522–528.
10. Pardeshi, V. A. S., Chundawat, N. S., Pathan, S. I., Sukhwal, P., Chundawat, T. P. S., and Singh, G. P. A review on synthetic approaches of benzimidazoles. Synthetic Communications. 2021; 51(4):485–513.
11. Chandrika, N. T., Shrestha, S. K., Ngo, H. X., and Garneau-Tsodikova, S. Synthesis and investigation of novel benzimidazole derivatives as antifungal agents. Bioorganic and Medicinal Chemistry. 2016; 24(16): 3680–3686.
12. Mavvaji, M., and Akkoc, S. Recent advances in the application of heterogeneous catalysts for the synthesis of benzimidazole derivatives. Coordination Chemistry Reviews. 2024; 505: 215714.
13. Abd El Salam HA, Abdelglil MI, Sabry E, Abdelraof M, Abdelwahed S, Gadallah MA, El-Rashedy AA, Saleh A, Srour AM. Rationale design, synthesis and antimicrobial activity of benzimidazole-pyridinecarbonitrile conjugates: Insights into ROS-induced oxidative damage and molecular dynamics simulations. Bioorganic Chemistry. 2025; 108627.
14. Chen, B., et al. Biomass-derived N-doped carbon materials with silica-supported ultrasmall ZnO nanoparticles: Robust catalysts for the green synthesis of benzimidazoles. Chemistry A European Journal. 2018; 24(14): 3481–3487.
15. Arvind Kumar Singh, Ekta Khare, Hridesh Singh Chauhan. Evaluation of Benzimidazole Derivatives by using Aldehydes. Research J. Pharm. and Tech. 2014; 7(6): 677-685.
16. Tyagi, A., Chauhan, M., Nain, S. An update on the green synthesis of benzimidazole scaffolds as antifungal agents. Pharm Chem J. 2024; 58(5): 816–827.
17. Kumar, J. R., Jawahar, J. L., and Pathak, D. P. Synthesis of benzimidazole derivatives: As anti-hypertensive agents. Journal of Chemistry. 2006; 3(4): 765712.
18. Ekta khare, G. Mariappan, Synthesis and Biological Evaluation of Benzimidazole. International Journal of Research in Pharmacy and Chemistry. 2018; 8(1): 61-68.
19. Ekta Khare, Pradeep Kashyap, Unnati Kushwaha. Design, Molecular Modelling and Synthesis of Antihypertensive Agent. Research J. Pharm. and Tech. 2020; 13(1): 101-105.
20. Klimešová, V., Koci, J., Pour, M., Stachel, J., Waisser, K., and Kaustová, J., Synthesis and preliminary evaluation of benzimidazole derivatives as antimicrobial agents. European Journal of Medicinal Chemistry, 2002; 37(5):409–418.
21. Amalesh Samanta, Aditya Kumar Jena, Chandrima Sinha, Soma Ghosh, Anurup Mandal. Antibacterial and Pharmacological Evaluation of Root Extract of Plant Achyranthes aspera (Amaranthaceae). Research J. Pharm. and Tech. 2010; 3(3): 910-914.
22. El harti Jaouad, Adouani Badr, Benmoussa Adnane, Ansar M’hammed, Taoufik Jamal. Benzimidazoles and Pharmacological Activities: A Review. Research J. Pharm. and Tech. 2014; 7(4): 481-488.
23. K. Girija, S. Karthika, Nisha Mathew. Synthesis and Anti-Microbial Activity of Some Novel Mannich Base Aryl Imidazole Derivatives. Research J. Pharm. and Tech. 2014; 7(9): 1025-1028.
24. Palled M. S.., Lohar V. R., Kalekar M. C., Patil P. B., Bhat A. R. Synthesis of 1,2,3,4-[1-N- Methyl Benzimidazole] 3-Phenyl Substituted Thiazolidine, 4-One and Carbohydrazide Derivatives for Antimicrobial Activity. Research J. Pharm. and Tech. 2012; 5(2): 249-252.
25. Nandini R Pai, Deepnandan S Dubhashi. Pharmacological Evaluation of Substituted Benzeneacetic Acid Ester Derivatives for Their Sedative, Antibacterial and Antifungal Potential. Research J. Pharm. and Tech. 2010; 3(2): 570-577.
26. Umesh Kumar, Rakesh Narang, Surendra Kumar Nayak, Sachin Kumar Singh, Vivek Gupta. Benzimidazole: Structure Activity Relationship and Mechanism of Action as Antimicrobial Agent. Research J. Pharm. and Tech. 2017; 10(7): 2400-2414.
27. Kartik Kaushik, Harsh Bhardwaj, Gyanendra Kumar Sharma. Synthesis and biological evaluations of some novel Benzimidazole Derivatives. Research J. Pharm. and Tech. 2020; 13(1): 368-372.
28. Pooja Kumari, Umakant, Gyanendra Sharma. Synthesis and Antibacterial activity of some newer Benzimidazole derivatives. Research J. Pharm. and Tech. 2020; 13(6): 2597-2600.
29. Nagenahalli JB, Reddiyappa P, K Thammaiah A. Synthesis of Pharmacologically Potent Benzimidazole Analogs. Polycyclic Aromatic Compounds. 2025; 45(1): 106-22.
30. Bai S, Zhang M, Tang S, Li M, Wu R, Wan S, Chen L, Wei X, Li F. Research progress on benzimidazole fungicides: A review. Molecules. 2024; 29(6): 1218.