A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold
Keywords:Benzimidazole, Mannich base, Schiff base, Antifungal activity, Anti-inflammatory activity, Anticancer activity
Background: Benzimidazole is a category of heterocyclic aromatic compounds formed from the fusion of six membered benzene with five membered imidazolering. The moiety possesses diverse biological and clinical applications. A number of studies have shown that a varied substituent around the benzimidazole nucleus results in pharmacologically active compounds of therapeutic interest.
Purpose: Owing to its number of pharmacological properties, this moiety is of choice of interest in designing and synthesis of new therapeutic compounds. The existence of the benzimidazole core in numerous groups of biological agents like antimicrobial, antiviral, antiparasitic, antihypertensive, anticancer, CNS stimulant as well as depressants has made important scaffold for development of many newer therapeutic agents. There is utmost need to understand the synthesis and associated role of benzimidazole derived compounds in different diseases. Therefore, in the present review, we attempt to discuss various derivatives of benzimidazole nucleus with different pharmacological activities.
Conclusion: Benzimidazoles have played a great role in discovery of drug and development. Huge attempt has been made towards benzimidazole heterocyclic-based organic compounds with great excellence that resulted in drugs with enormous biological activity. Therapeutic drugs containing benzimidazole nucleus are used in building drugs that serve to be an active area of research. This article becomes a source that will lead to discovery of new opportunities for all researchers interested in benzimidazole-based heterocyclic medicinal chemistry.
Alaqeel, S.I. (2017). Synthetic approach to benzimidazole from ortho phenylenediamine. Journal of Saudi Chemical Society, 21(2), 229-237. https://doi.org/10.1016/j.jscs.2016.08.001
Anand, K., & Wakode, S. (2017). Development of drugs based on Benzimidazole Heterocycle: recent advancement and insights. International Journal of Chemical Studies, 5(2), 350-362.
Anandarajagopal, K., Tiwari, R.N., Bothara, K.G., Sunilson, J.A.J., Dineshkumar, C., & Promwichit, P. (2010). 2-Mercaptobenzimidazole derivatives: Synthesis and Anticonvulsant activity. Advances in Applied Science Research, 1(2), 132-138.
Bhatt, H.G., Agarwal, Y.K., Raval, H.G., Manna, K., & Desai, P.R. (2010). Histamine H4 receptor: A novel therapeutic target for immune and allergic responses. Mini Reviews in Medicinal Chemistry, 10(14), 1293-1308. https://doi.org/10.2174/138955710793564124
Chaudhari, V.K., Pathak, D., & Singh, S. (2014). Benzimidazole: As potential biologically active agent. International Research Journal of Pharmacy, 5(12), 861-875. https://doi.org/10.7897/2230-8407.0512176
Coruzzi, G., Adami, M., Guaita, E., de Esch I.J.P., & Leurs, R. (2007). Anti-inflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists in a rat model of carrageenan-induced acute inflammation. European Journal of Pharmacology, 563(1-3), 240-244. https://doi.org/10.1016/j.ejphar.2007.02.026
Enumula, S., Pangal, A., Gazge, M., Shaikh, J.A., & Ahmed, K. (2014). Diverse Pharmacological aspects of Benzimidazole Derivatives. Research Journal of Chemical Sciences, 4(4), 78-88.
Gaba, M., Singh, S., & Mohan, C. (2014). Benzimidazole: An emerging scaffold for analgesics and anti-inflammatory agents. European Journal of Medicinal Chemistry, 76, 494-505. https://doi.org/10.1016/j.ejmech.2014.01.030
Gaud, V.M., Sreenivasulu, N., Rao, A.S., & Chigiri, S. (2011). Synthesis antimicrobial and pharmacological evaluation of substituted benzimidazole. Der Pharma Chemica, 3(1), 446-452.
Kapoor, A., & Dhiman, N. (2016). Anticancer evaluation of 2-aryl substituted benzimidazole derivatives bearing1,3,4-oxadiazole nucleus. Der Pharmacia Lettre, 8(12), 149-156.
Kumar, D., & Sharma, K. (2012). A Versatile Analogue of benzimidazole. International Journal of Pharmacy Professional, 13-15.
Marriappan, G., Bhuvyan, N.R., Kumar, P., Kumar, D., & Murali, K. (2009). Synthesis and biological evaluation of mannich bases of benzimidazole derivatives. Indian Journal of Chemistry - Section B (IJC-B), 50B(09), 1216-1219.
Morcoss, M.M., Abdelhafez, El S.M.N., Abdel-Rahman, H.M., Abdel-Aziz, M., & El-Ella, D.A.A. (2020). Novel Benzimidazole derivatives as promising anticancer lead compounds: Design Synthesis and Molecular docking study. Journal of Advanced Biomedical and Applied Pharmaceutical Sciences, 3(2), 45-52. https://doi.org/10.21608/jabps.2020.21160.1064
Özkay, Y., & Karacr, H. (2011). Antimicrobial activity of a new combination system of benzimidazole and various azoles. Archiv der Pharmazie, 344(4), 264-271. https://doi.org/10.1002/ardp.201000172
Palit, R., Kumar, R., Saraswat, N., Wal, A., & Upadhaya, P.K. (2016). Benzimidazole: An Overview International Journal of Research and Ayurveda Pharmacy, 7(6), 2277-4343. https://doi.org/10.7897/2277-4343.076243
Salahuddin, Shaharyar, M., & Mazumdera, A. (2017). Benzimidazoles: A biologically active compounds. Arabian Journal of Chemistry, 10(S1), S157-S173. https://doi.org/10.1016/j.arabjc.2012.07.017
Sethi, R., Arora, S., Saini, D., & Jain, S. (2016). Synthesis, characterization, molecular docking studies and antimicrobial evaluation of N-benzimidazol-1-yl methyl benzamide derivatives. Indian Journal of Pharmaceutical Education and Research, 50(3), 424-434. https://doi.org/10.5530/ijper.50.3.16
Sethi, R., Jain, S., Arora, S., Saini, D., & Jain, N. (2018). Synthesis, characterization and molecular docking studies of novel N-(benzimidazol-1-ylmethyl)-4-chlorobenzamide analogues for potential anti-inflammatory and antimicrobial activity. Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry, 17(1), 16-31. https://doi.org/10.2174/1871523017666180426125141
Sharma, A., Luxami, V., & Paul, K. (2014). Synthesis, single crystal and antitumor activities of benzimidazole–quinazoline hybrids. Bioorganic and Medicinal Chemistry letters, 24(2), 624-629. https://doi.org/10.1016/j.bmcl.2013.12.005
Sharma, D., Narasimhan, B., Kumar, P., Judge, V., Narang, R., De Clercq, E., & Balzarini, J. (2009). Synthesis and antimicrobial and antiviral activity of substituted benzimidazoles. Journal of Enzyme Inhibition and Medicinal Chemistry, 24(5), 1161-1168. https://doi.org/10.1080/14756360802694427
Singh, V., & Parle, A. (2020). Synthesis characterization and antioxidant activity of 2-aryl benzimidazole derivatives. Asian Journal of Pharmaceutical Research and Development, 8(2), 35-44. https://doi.org/10.22270/ajprd.v8i2.582
Singh, N., Pandurangan, A., Rana, K., Anand, P., Ahamad, A., & Tiwari, A.K. (2012). Benzimidazole: A short review of their antimicrobial activities. International Current Pharmaceutical Journal, 1(5), 119-127. https://doi.org/10.3329/icpj.v1i5.10284
Singh, V.K., & Parle, V. (2019). The Intriguing Benzimidazole: A Review. International Journal of Pharmaceutical Sciences and Research, 1(5), 1540-1552. https://doi.org/10.13040/IJPSR.0975-8232.10(4).1540-52
Tahlan, S., Kumar, S., & Narasimhan, B. (2019). Antimicrobial potential of 1H-benzo[d]imidazole scaffold. Bio Medicinal Chemistry, 13(18), 1-27. https://doi.org/10.1186/s13065-019-0521-y
Tewari, A.K., & Mishra, A. (2005). Synthesis and antiviral activities of N-substituted-benzimidazole derivatives. Indian Journal of Chemistry, 45B, 489-493.
Vasil’ev, P.M., Kalitin, K.Yu., Spasov, A.A., Grechko, O.Yu., Poroikov, V.V., Filimon, D.A., & Anisimova, V.A. (2015). Study of anticonvulsant properties of benzimidazole derivatives. Pharmaceutical Chemistry Journal, 50, 775–780. https://doi.org/10.1007/s11094-017-1530-6
Walia, R., Naaz, S., Iqbal, K., Lamba, H., & Hedaitullah, M. (2011). Benzimidazole derivatives- An Overview. International Journal of Research and Pharmacy, 1(3), 565-574.
How to Cite
Copyright (c) 2020 Swikriti, Sandeep Arora and Ritchu Babbar
This work is licensed under a Creative Commons Attribution 4.0 International License.
Articles in Journal of Pharmaceutical Technology, Research And Management (J. Pharm. Technol. Res. Manag.) by Chitkara University Publications are Open Access articles that are published with licensed under a Creative Commons Attribution- CC-BY 4.0 International License. Based on a work at https://jptrm.chitkara.edu.in. This license permits one to use, remix, tweak and reproduction in any medium, even commercially provided one give credit for the original creation.
View Legal Code of the above mentioned license, https://creativecommons.org/licenses/by/4.0/legalcode
View Licence Deed here https://creativecommons.org/licenses/by/4.0/
|Journal of Pharmaceutical Technology, Research And Management by Chitkara University Publications is licensed under a Creative Commons Attribution 4.0 International License.
Based on a work at https://jptrm.chitkara.edu.in