Skip to content
2000
image of Exploring the Pharmacological Profiles of Benzimidazole Derivatives: A Comprehensive Review

Abstract

Fused heterocyclic scaffolds appear to be the most developing topic in therapeutic chemistry, especially benzimidazole, is a bicyclic compound consisting of a benzene ring fused to an imidazole ring and found in the tissues of plants and animals (including histidine, purines, and vitamin B12). Also, it plays an important structural role in the preparation of bioactive compounds. Derivatives of benzimidazole have shown therapeutic activity in various applications, including anthelmintic, anti-inflammatory, anticancer, antimicrobial, and antiulcer. The physicochemical properties of benzimidazole have evolved to promote this activity mainly because of their favourable physical features and their ability to function on several functional biological targets. They include hydrogen bonding, π–π stacking, and hydrophobic interactions. More recently, molecular docking studies with their binding affinity and mechanism of action have become known, which further contributes to the rational design of novel drugs. Derivatives of benzimidazole seem to hold considerable potential for multitargeted therapeutic strategies. In this review, we offer an overview of the chemistry, latest biological activities, design techniques, and structure–activity relationship (SAR) data of several analogues derived from benzimidazole.

© 2026 Bentham Science Publishers
Loading

Article metrics loading...

/content/journals/ctmc/10.2174/0115680266425342260112130801
2026-03-04
2026-03-08

  • From This Site

    /content/journals/ctmc/10.2174/0115680266425342260112130801
    dcterms_title,dcterms_subject,pub_keyword
    -contentType:Contributor -contentType:Concept -contentType:Institution
    10
    5
Loading full text...

Full text loading...

References

  1. Ebenezer O. Oyetunde-Joshua F. Omotoso O.D. Shapi M. Benzimidazole and its derivatives: Recent Advances (2020–2022). Results Chem. 2023 5 100925 10.1016/j.rechem.2023.100925
    [Google Scholar]
  2. Patel M. Avashthi G. Gacem A. Alqahtani M.S. Park H.K. Jeon B.H. A review of approaches to the metallic and non-metallic synthesis of benzimidazole (BnZ) and their derivatives for biological efficacy. Molecules 2023 28 14 5490 10.3390/molecules28145490 37513362
    [Google Scholar]
  3. Basha N.J. Therapeutic efficacy of benzimidazole and its analogs: An update. Polycycl. Aromat. Compd. 2023 43 7 6549 6569 10.1080/10406638.2022.2118334
    [Google Scholar]
  4. Mahurkar N.D. Gawhale N.D. Lokhande M.N. Uke S.J. Kodape M.M. Benzimidazole: A versatile scaffold for drug discovery and beyond – A comprehensive review of synthetic approaches and recent advancements in medicinal chemistry. Results Chem. 2023 6 101139 10.1016/j.rechem.2023.101139
    [Google Scholar]
  5. Monga J. Ghosh N.S. Rani I. Singh R. Deswal G. Dhingra A.K. Grewal A.S. Unlocking the pharmacological potential of benzimidazole derivatives: A pathway to drug development. Curr. Top. Med. Chem. 2024 24 5 437 485 10.2174/0115680266283641240109080047 38311918
    [Google Scholar]
  6. Sharma S. Gupta M. Gupta M. Sahu J.K. Significance of Benzimidazole analogues for the creation of novel molecules in drug discovery. Curr. Chem. Lett. 2023 12 1 27 44 10.5267/j.ccl.2022.9.008
    [Google Scholar]
  7. Kavya G. Sivan A. Exploring the versatility of benzimidazole scaffolds as medicinal agents: A brief update. Benzimidazole IntechOpen 2022 10.5772/intechopen.101942
    [Google Scholar]
  8. Wu K. Peng X. Chen M. Li Y. Tang G. Peng J. Peng Y. Cao X. Recent progress of research on anti‐tumor agents using benzimidazole as the structure unit. Chem. Biol. Drug Des. 2022 99 5 736 757 10.1111/cbdd.14022 35064629
    [Google Scholar]
  9. Fadel M.A. Ali D.S. Mousa H.K. Synthesis and characterization of new benzimidazole-nitrone derivatives and study of their effect as anti-fungal. Al-Qadisiyah J. Pure Sci. 2022 27 1 26 10.29350/2411‑3514.1222
    [Google Scholar]
  10. Gharat K. Ghara A. Patil K. Mokal P. Shaikh S.F. An overview of the bioactive properties of benzimidazole derivatives. Int. J. Adv. Res. Sci. Commun. Technol 2025 5 10 171 176 10.48175/IJARSCT‑24731
    [Google Scholar]
  11. Nardi M. Cano N.C.H. Simeonov S. Bence R. Kurutos A. Scarpelli R. Wunderlin D. Procopio A. A review on the Green synthesis of benzimidazole derivatives and their pharmacological activities. Catalysts 2023 13 2 392 10.3390/catal13020392
    [Google Scholar]
  12. Bartholomew G.L. Kim S.F. Oyamada Y. Sbordone F. Carroll J.A. Jurczyk J.E. Yeung C.S. Barner-Kowollik C. Sarpong R. Phototransposition of indazoles to benzimidazoles: Tautomer‐dependent reactivity, wavelength dependence, and continuous flow studies. Angew. Chem. Int. Ed. 2025 64 31 e202423803 10.1002/anie.202423803 39899448
    [Google Scholar]
  13. Faheem M. Rathaur A. Pandey A. Kumar Singh V. Tiwari A.K. A review on the modern synthetic approach of benzimidazole candidate. ChemistrySelect 2020 5 13 3981 3994 10.1002/slct.201904832
    [Google Scholar]
  14. Thapa S. Nargund S.L. Biradar M.S. Banerjee J. Karati D. In-silico investigation and drug likeliness studies of benzimidazole congeners: The new face of innovation. Inform. Med. Unlocked 2023 38 101213 10.1016/j.imu.2023.101213
    [Google Scholar]
  15. Guo Y. Hou X. Fang H. Recent applications of benzimidazole as a privileged scaffold in drug discovery. Mini Rev. Med. Chem. 2020 21 11 1367 1379 10.2174/1389557520666200804124924 32753010
    [Google Scholar]
  16. Law C.S.W. Yeong K.Y. Benzimidazoles in drug discovery: A patent review. ChemMedChem 2021 16 12 1861 1877 10.1002/cmdc.202100004 33646618
    [Google Scholar]
  17. Luo J. Jin Y. Li X. Luo L. Zuo Z. Liu X. Revealing packing structure in benzimidazole-containing polyimides: Anti-parallel offset π-π stacking. Polymer 2024 302 127056 10.1016/j.polymer.2024.127056
    [Google Scholar]
  18. Li H. Gao C. Li Z. Guo Y. Cao S. Zhao Y. Structural insight into imidazopyridines and benzimidazoles: The importance of the hydrogen bond, π-stacking interactions and intramolecular charge transfer effect for fluorescence. CrystEngComm 2024 26 38 5380 5392 10.1039/D4CE00714J
    [Google Scholar]
  19. Khan Y. Rehman W. Hussain R. Khan S. Malik A. Khan M. Liaqat A. Rasheed L. Begum F. Fazil S. Khan I. Abdellatif M.H. New biologically potent benzimidazole‐based‐triazole derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors along with molecular docking study. J. Heterocycl. Chem. 2022 59 12 2225 2239 10.1002/jhet.4553
    [Google Scholar]
  20. Ahmad N. Azad M.I. Khan A.R. Azad I. Benzimidazole as a promising antiviral heterocyclic scaffold: A review. J. Sci. Arts 2021 21 1 273 284 10.46939/J.Sci.Arts‑21.1‑b05
    [Google Scholar]
  21. Kumar R. Marianesan A.B. Pathak S. Benzimidazole as a privileged scaffold in drug design and discovery. Curr. Top. Med. Chem. 2024 24 17 1504 1528 10.2174/0115680266314704240522112439 38818908
    [Google Scholar]
  22. Veerasamy R. Roy A. Karunakaran R. Rajak H. Structure–activity relationship analysis of benzimidazoles as emerging anti-inflammatory agents: An overview. Pharmaceuticals 2021 14 7 663 10.3390/ph14070663 34358089
    [Google Scholar]
  23. Oon C.E. Subramaniam A.V. Ooi L.Y. Yehya A.H.S. Lee Y.T. Kaur G. Sasidharan S. Qiu B. Wang X. BZD9L1 benzimidazole analogue hampers colorectal tumor progression by impeding angiogenesis. World J. Gastrointest. Oncol. 2023 15 5 810 827 10.4251/wjgo.v15.i5.810 37275453
    [Google Scholar]
  24. Aragón-Muriel A. Liscano Y. Morales-Morales D. Polo-Cerón D. Oñate-Garzón J. A study of the interaction of a new benzimidazole Schiff base with synthetic and simulated membrane models of bacterial and mammalian membranes. Membranes 2021 11 6 449 10.3390/membranes11060449 34208443
    [Google Scholar]
  25. Ali A.M. Tawfik S.S. Mostafa A.S. Massoud M.A.M. Benzimidazole‐based protein kinase inhibitors: Current perspectives in targeted cancer therapy. Chem. Biol. Drug Des. 2022 100 5 656 673 10.1111/cbdd.14130 35962624
    [Google Scholar]
  26. Singh K. Bhushan B. Varma A.K. Shekhar R. Sharma R.K. Ghosh N.S. Pandey E. Saha S. Kumar S. Mishra A.K. Agrawal M. A comprehensive review of the benzimidazole scaffold as a potential nucleus for anti-ulcer activity. Lett. Org. Chem. 2024 21 6 493 504 10.2174/0115701786267759231121070546
    [Google Scholar]
  27. Begunov R.S. Egorov D.O. Chetvertakova A.V. Savina L.I. Zubishina A.A. Antibacterial activity of the halogen- and Nitro derivatives of benzimidazole against Bacillus subtilis. Antibiot. Khimioter. 2023 68 3-4 19 24 10.37489/0235‑2990‑2023‑68‑3‑4‑19‑24
    [Google Scholar]
  28. Türkan F. Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes. Arch. Physiol. Biochem. 2021 127 2 97 101 10.1080/13813455.2019.1618341 31135232
    [Google Scholar]
  29. Wagih N. Abdel-Rahman I.M. El-Koussi N.A. El-Din A. Abuo-Rahma G. Abuo-Rahma G. Anticancer benzimidazole derivatives as inhibitors of epigenetic targets: A review article. RSC Advances 2025 15 2 966 1010 10.1039/D4RA05014B 39807197
    [Google Scholar]
  30. Tong J.B. Feng Y. Luo D. Wang T.H. 6-amide-2-aryl benzoxazole/benzimidazole derivatives as VEFGR-2 inhibitors in two-and three-dimensional QSAR studies: Topomer CoMFA and HQSAR. Chem. Pap. 2021 75 7 3551 3562 10.1007/s11696‑021‑01588‑w
    [Google Scholar]
  31. Timoudan N. Al-Gorair A.S. El Foujji L. Warad I. Safi Z. Dikici B. Benhiba F. Qaiss A.E.K. Bouhfid R. Bentiss F. Al-Juaid S.S. Abdallah M. Zarrouk A. Corrosion inhibition performance of benzimidazole derivatives for protection of carbon steel in hydrochloric acid solution. RSC Advances 2024 14 41 30295 30316 10.1039/D4RA05070C 39315030
    [Google Scholar]
  32. Rashid M. Benzimidazole molecule as new anticancer agent; Design, synthesis and admet prediction. J. Chil. Chem. Soc. 2021 66 5164 5182 10.4067/S0717‑97072021000205164
    [Google Scholar]
  33. Rashid M. Afzal O. Altamimi A.S.A. Benzimidazole molecule hybrid with oxadiazole ring as antiproliferative agents: In-silico analysis, synthesis and biological evaluation. J. Chil. Chem. Soc. 2021 66 2 5164 5182 10.4067/S0717‑97072021000205164
    [Google Scholar]
  34. Roy S. Basak S. Roy S. Dey P. Barman H. Singh B. Sarkar K. Sen S. Das R.K. Debnath S. Biswas G. Design, synthesis, molecular docking, pharmacokinetic properties, and molecular dynamics simulation of sulfonyl derivatives of benzimidazole against Parkinson’s disease. Curr. Med. Chem. 2024 32 10.2174/0109298673337912241007120510 39449335
    [Google Scholar]
  35. Basuri P. Gonzalez L.E. Morato N.M. Pradeep T. Cooks R.G. Accelerated microdroplet synthesis of benzimidazoles by nucleophilic addition to protonated carboxylic acids. Chem. Sci. 2020 11 47 12686 12694 10.1039/D0SC02467H 34094463
    [Google Scholar]
  36. Belkharchach S. Ighachane H. Rochdi A. Ait Ali M. Lazrek H.B. One-pot synthesis of benzimidazoles using H2SO4@HTC as catalyst. Org. Prep. Proced. Int. 2021 53 3 268 277 10.1080/00304948.2021.1873066
    [Google Scholar]
  37. Huang H.Y. Lin X.Y. Yen S.Y. Liang C.F. Facile access to N-formyl imide as an N-formylating agent for the direct synthesis of N-formamides, benzimidazoles and quinazolinones. Org. Biomol. Chem. 2020 18 29 5726 5733 10.1039/D0OB01080D 32666985
    [Google Scholar]
  38. Bermejo-López A. Carrasco S. Tortajada P.J. Kopf K.P.M. Sanz-Marco A. Hvid M.S. Lock N. Martín-Matute B. Selective synthesis of imines by photo-oxidative Amine cross-condensation catalyzed by PCN-222(pd). ACS Sustain. Chem.& Eng. 2021 9 43 14405 14415 10.1021/acssuschemeng.1c04389
    [Google Scholar]
  39. Dehbanipour Z. Zarnegareyan A. Magnetic nanoparticles supported a palladium bis(benzothiazole) complex: A novel efficient and recyclable catalyst for the synthesis of benzimidazoles and benzothiazoles from benzyl alcohol. SSRN Electron. J 2022 10.2139/ssrn.4031591
    [Google Scholar]
  40. Naeimi H. Alishahi N. An efficient and one-pot reductive cyclization for synthesis of 2-substituted benzimidazoles from o-nitroaniline under microwave conditions. J. Ind. Eng. Chem. 2014 20 4 2543 2547 10.1016/j.jiec.2013.10.038
    [Google Scholar]
  41. Xie Z. Zhou F. Ding K. Copper‐mediated diamination of arylboronic acids for the synthesis of 2‐aryl benzimidazoles using trimethylsilyl azide as the amino sources with aldehydes. Adv. Synth. Catal. 2020 362 16 3442 3446 10.1002/adsc.202000385
    [Google Scholar]
  42. Li M. Tang Y. Gao H. Rao G. Mao Z. Efficient cu‐catalyzed synthesis of benzimidazoles using ammonia as nitrogen source in water. Asian J. Org. Chem. 2020 9 7 1027 1031 10.1002/ajoc.202000236
    [Google Scholar]
  43. Kadu V.R. Chavan H.V. Gholap S.S. Additive free greener synthesis of 1,2-disubstituted benzimidazoles using aqueous extract of acacia concinna pods as an efficient surfactant type catalyst. Polycycl. Aromat. Compd. 2021 41 6 1263 1273 10.1080/10406638.2019.1670219
    [Google Scholar]
  44. Marri M.R. Peraka S. Macharla A.K. Mameda N. Kodumuri S. Nama N. Catalyst-free one-pot synthesis of benzimidazoles from 1,2-diaminoarenes and alcohols. Tetrahedron Lett. 2014 55 48 6520 6525 10.1016/j.tetlet.2014.09.081
    [Google Scholar]
  45. Natarajan R. Kumar P. Subramani A. Siraperuman A. Angamuthu P. Bhandare R.R. Shaik A.B. A critical review on therapeutic potential of benzimidazole derivatives: A privileged scaffold. Med. Chem. 2024 20 3 311 351 10.2174/0115734064253813231025093707 37946342
    [Google Scholar]
  46. Kumar P. Bhatia R. Rangra N.K. Scaffolds imparting anthelmintic activity: Recent advancements and SAR studies. Mol. Divers. 2025 29 1 783 816 10.1007/s11030‑024‑10869‑x 39083219
    [Google Scholar]
  47. Kar N.R. Samathoti P. Muralitharan S. Mishra S.R. Current trends, modern synthetic approach, SAR and biological activities of benzimidazole derivatives. Community Pract. 2023 20 6 21 10.5281/zenodo.8339770
    [Google Scholar]
  48. Elmaaty A.A. Darwish K.M. Chrouda A. Boseila A.A. Tantawy M.A. Elhady S.S. Shaik A.B. Mustafa M. Al-karmalawy A.A. In silico and in vitro studies for benzimidazole anthelmintics repurposing as VEGFR-2 antagonists: Novel mebendazole-loaded mixed micelles with enhanced dissolution and anticancer activity. ACS Omega 2022 7 1 875 899 10.1021/acsomega.1c05519 35036753
    [Google Scholar]
  49. Bhavsar Z.A. Acharya P.T. Jethava D.J. Patel H.D. Recent advances in development of anthelmintic agents: Synthesis and biological screening. Synth. Commun. 2020 50 7 917 946 10.1080/00397911.2019.1695276
    [Google Scholar]
  50. Jang J. Koh B. Lee K. Discovery of benzimidazole-2-amide BNZ-111 as new tubulin inhibitor. Bioorg. Med. Chem. Lett. 2024 113 129953 10.1016/j.bmcl.2024.129953 39270806
    [Google Scholar]
  51. Bano S. Nadeem H. Zulfiqar I. Shahzadi T. Anwar T. Bukhari A. Masaud S.M. Synthesis and anti-inflammatory activity of benzimidazole derivatives; an in vitro, in vivo and in silico approach. Heliyon 2024 10 9 e30102 10.1016/j.heliyon.2024.e30102 38726192
    [Google Scholar]
  52. Farag B. Zaki M.E.A. Elsayed D.A. Gomha S.M. Benzimidazole chemistry in oncology: Recent developments in synthesis, activity, and SAR analysis. RSC Advances 2025 15 23 18593 18647 10.1039/D5RA01077B 40463335
    [Google Scholar]
  53. Poddar S.K. Saha P. Spriha S.E. Abdur Rahman S.M. Synthesis, in vivo and in silico evaluation of analgesic, anti‐inflammatory and antidiarrheal activities of benzimidazole derivatives. ChemistrySelect 2025 10 9 e202401267 10.1002/slct.202401267
    [Google Scholar]
  54. Joseph J. Perumal P. Francis P. Synthesis and anti-inflammatory screening of various benzimidazole derivatives. Res. J. Pharm. Technol 2016 9 9 1329 10.5958/0974‑360X.2016.00253.5
    [Google Scholar]
  55. Hagar F.F. Abbas S.H. Atef E. Abdelhamid D. Abdel-Aziz M. Benzimidazole scaffold as a potent anticancer agent with different mechanisms of action (2016–2023). Mol. Divers. 2025 29 2 1821 1849 10.1007/s11030‑024‑10907‑8 39031290
    [Google Scholar]
  56. Satija G. Sharma B. Madan A. Iqubal A. Shaquiquzzaman M. Akhter M. Parvez S. Khan M.A. Alam M.M. Benzimidazole based derivatives as anticancer agents: Structure activity relationship analysis for various targets. J. Heterocycl. Chem. 2022 59 1 22 66 10.1002/jhet.4355
    [Google Scholar]
  57. Wagh D.D. Kankate R.S. Benzimidazole derivatives in anticancer therapy: A comprehensive review. Biosci. Biotechnol. Res. Asia 2025 22 3 849 863 10.13005/bbra/3409
    [Google Scholar]
  58. Akhtar M.J. Yar M.S. Sharma V.K. Khan A.A. Ali Z. Haider M.D.R. Pathak A. Recent progress of benzimidazole hybrids for anticancer potential. Curr. Med. Chem. 2020 27 35 5970 6014 10.2174/0929867326666190808122929 31393240
    [Google Scholar]
  59. Barasa L. Vemana H.P. Surubhotla N. Ha S.S. Kong J. Yong A. Croft J.L. Dukhande V.V. Yoganathan S. Synthesis and biological evaluation of structurally diverse benzimidazole scaffolds as potential chemotherapeutic agents. Anticancer. Agents Med. Chem. 2020 20 3 301 314 10.2174/1871520619666191028101506 31746304
    [Google Scholar]
  60. Yadav B. Design and synthesis of novel benzimidazole derivatives as antimicrobial agents. Indian J. Pharm. Chem. Analyt Techniq 2025 1 1 13
    [Google Scholar]
  61. Mohapatra T.R. Ganguly S. Ghosh R. Choowngkomon K. Design, synthesis, and structure–activity relationship (SAR) studies of novel disubstituted benzimidazole derivatives as potential anti‐HIV and antimicrobial agents. ChemistrySelect 2025 10 28 e00615 10.1002/slct.202500615
    [Google Scholar]
  62. Marinescu M. Synthesis of antimicrobial benzimidazole–pyrazole compounds and their biological activities. Antibiotics 2021 10 8 1002 10.3390/antibiotics10081002 34439052
    [Google Scholar]
  63. de Lócio L.L. do Nascimento A.P.S. Santos M.B. Gomes J.N.S. de Medeiros e Silva, Y.M.S.; Albino, S.L.; dos Santos, V.L.; de Moura, R.O. Application of heterocycles as an alternative for the discovery of new anti-ulcer compounds: A mini-review. Curr. Pharm. Des. 2022 28 17 1373 1388 10.2174/1381612828666220512095559 35549862
    [Google Scholar]
  64. Pinelli A. Trivulzio S. Malvezzi L. Rossoni G. Beretta L. 2-substituted derivatives of benzimidazole inhibiting gastric acid secretion in rats. Arzneimittelforschung 1989 39 4 467 469 2751732
    [Google Scholar]
  65. Tajane P.S. Sawant R.L. updated review on benzimidazole derivatives as potential antihypertensive agents. Int. J. Health Sci. 2022 ••• 7169 7179 10.53730/ijhs.v6nS1.6543
    [Google Scholar]
  66. Bhat R.M. Hegde V. Budagumpi S. Adimule V. Keri R.S. Benzimidazole-oxadiazole hybrids-development in medicinal chemistry: An overview. Chem. Biol. Drug Des. 2024 104 2 e14609 10.1111/cbdd.14609 39155152
    [Google Scholar]
  67. Kumar S. Bhatt A. Kant R. Biological significance of benzimidazole derivatives: A review. Chem. Biol. Interact. 2021 11 6 197
    [Google Scholar]
  68. Alheety M.A. Mohammed L.A. Farhan M.A. Dadoosh S.A. Majeed A.H. Mahmood A.S. Mahmoud Z.H. A review on benzimidazole heterocyclic compounds: Synthesis and their medicinal activity applications. SynOpen 2023 7 4 652 673 10.1055/a‑2155‑9125
    [Google Scholar]
  69. Yang H. Ren Y. Gao X. Gao Y. Synthesis and anticoagulant bioactivity evaluation of 1,2,5-trisubstituted benzimidazole fluorinated derivatives. Chem. Res. Chin. Univ. 2016 32 6 973 978 10.1007/s40242‑016‑6205‑4
    [Google Scholar]
  70. Başaran R. Kilcigi̇l G. Eke B. Evaluation of the antioxidant activity of some imines containing 1H-benzimidazoles. Turk. J. Pharm. Sci. 2020 17 6 626 630 10.4274/tjps.galenos.2019.05914 33389952
    [Google Scholar]
  71. Baldisserotto A. Demurtas M. Lampronti I. Tacchini M. Moi D. Balboni G. Vertuani S. Manfredini S. Onnis V. In-vitro evaluation of antioxidant, antiproliferative and photo-protective activities of benzimidazolehydrazone derivatives. Pharmaceuticals 2020 13 4 68 10.3390/ph13040068 32326658
    [Google Scholar]
  72. Escala N. Valderas-García E. Álvarez Bardón M. de Agüero V.C.G. López-Pérez J.L. Rojo-Vázquez F.A. Feliciano A.S. Martínez-Valladares M. Balaña-Fouce R. del Olmo E. Further and new target-based benzimidazole anthelmintics active against Teladorsagia circumcincta. J. Mol. Struct. 2022 1269 133735 10.1016/j.molstruc.2022.133735
    [Google Scholar]
  73. Sawant R. Kawade D. Synthesis and biological evaluation of some novel 2-phenyl benzimidazole-1-acetamide derivatives as potential anthelmintic agents. Acta Pharm. 2011 61 3 353 361 10.2478/v10007‑011‑0029‑z 21945914
    [Google Scholar]
  74. Kaliyaperumal S. Pattanayak P. Synthesis, characterization and in vitro evaluation for antimicrobial and anthelmintic activity of novel benzimidazole substituted 1,3,4-thiadiazole Schiff ’s bases 2021. FABAD J. Pharm. Sci. 2021 46 261
    [Google Scholar]
  75. Anichina K. Argirova M. Tzoneva R. Uzunova V. Mavrova A. Vuchev D. Popova-Daskalova G. Fratev F. Guncheva M. Yancheva D. 1H-benzimidazole-2-yl hydrazones as tubulin-targeting agents: Synthesis, structural characterization, anthelmintic activity and antiproliferative activity against MCF-7 breast carcinoma cells and molecular docking studies. Chem. Biol. Interact. 2021 345 109540 10.1016/j.cbi.2021.109540 34139148
    [Google Scholar]
  76. Valderas-García E. Häberli C. Álvarez-Bardón M. Escala N. Castilla-Gómez de Agüero V. de la Vega J. del Olmo E. Balaña-Fouce R. Keiser J. Martínez-Valladares M. Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus. Parasit. Vectors 2022 15 1 243 10.1186/s13071‑022‑05347‑y 35804427
    [Google Scholar]
  77. Kaur G. Silakari O. Benzimidazole scaffold based hybrid molecules for various inflammatory targets: Synthesis and evaluation. Bioorg. Chem. 2018 80 24 35 10.1016/j.bioorg.2018.05.014 29864685
    [Google Scholar]
  78. Arora R.K. Kaur N. Bansal Y. Bansal G. Novel coumarin–benzimidazole derivatives as antioxidants and safer anti-inflammatory agents. Acta Pharm. Sin. B 2014 4 5 368 375 10.1016/j.apsb.2014.07.001 26579406
    [Google Scholar]
  79. Thakurdesai P.A. Wadodkar S.G. Chopade C.T. Synthesis and anti-inflammatory activity of some benzimidazole-2-carboxylic acids. Pharmacologyonline 2007 1 314 329
    [Google Scholar]
  80. Achar K.C.S. Hosamani K.M. Seetharamareddy H.R. In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives. Eur. J. Med. Chem. 2010 45 5 2048 2054 10.1016/j.ejmech.2010.01.029 20133024
    [Google Scholar]
  81. Moharana A.K. Dash R.N. Mahanandia N.C. Subudhi B.B. Synthesis and anti-inflammatory activity evaluation of some benzimidazole derivatives. Pharm. Chem. J. 2022 56 8 1070 1074 10.1007/s11094‑022‑02755‑3 36405379
    [Google Scholar]
  82. Hussain A. AlAjmi M.F. Rehman M.T. Khan A.A. Shaikh P.A. Khan R.A. Evaluation of transition metal complexes of benzimidazole-derived scaffold as promising anticancer chemotherapeutics. Molecules 2018 23 5 1232 10.3390/molecules23051232 29883398
    [Google Scholar]
  83. Abbade Y. Kisla M.M. Hassan M.A.K. Celik I. Dogan T.S. Mutlu P. Ates-Alagoz Z. Synthesis, anticancer activity, and in silico modeling of alkylsulfonyl benzimidazole derivatives: Unveiling potent Bcl-2 inhibitors for breast cancer. ACS Omega 2024 9 8 9547 9563 10.1021/acsomega.3c09411 38434899
    [Google Scholar]
  84. Shrivastava N. Naim M.J. Alam M.J. Nawaz F. Ahmed S. Alam O. Benzimidazole scaffold as anticancer agent: Synthetic approaches and structure-activity relationship. Arch. Pharm. 2017 350 6 e201700040 10.1002/ardp.201700040 28544162
    [Google Scholar]
  85. Hsieh C.Y. Ko P.W. Chang Y.J. Kapoor M. Liang Y.C. Chu H-L. Lin H-H. Horng J-C. Hsu M-H. Design and synthesis of benzimidazole-chalcone derivatives as potential anticancer agents. Molecules 2019 24 18 3259 10.3390/molecules24183259 31500191
    [Google Scholar]
  86. Diaconu D. Antoci V. Mangalagiu V. Amariucai-Mantu D. Mangalagiu I.I. Quinoline–imidazole/benzimidazole derivatives as dual-/multi-targeting hybrids inhibitors with anticancer and antimicrobial activity. Sci. Rep. 2022 12 1 16988 10.1038/s41598‑022‑21435‑6 36216981
    [Google Scholar]
  87. Shaldam M.A. Hendrychová D. El-Haggar R. Vojáčková V. Majrashi T.A. Elkaeed E.B. Masurier N. Kryštof V. Tawfik H.O. Eldehna W.M. 2,4-Diaryl-pyrimido[1,2-a]benzimidazole derivatives as novel anticancer agents endowed with potent anti-leukemia activity: Synthesis, biological evaluation and kinase profiling. Eur. J. Med. Chem. 2023 258 115610 10.1016/j.ejmech.2023.115610 37437350
    [Google Scholar]
  88. Çevik U.A. Celik I. Görgülü Ş. Şahin İnan Z.D. Bostancı H.E. Karayel A. Özkay Y. Kaplancıklı Z.A. Novel benzimidazole-oxadiazole derivatives as anticancer agents with VEGFR2 inhibitory activity: Design, synthesis, in vitro anticancer evaluation, and in silico studies. ACS Omega 2025 10 7 6801 6813 10.1021/acsomega.4c08885 40028103
    [Google Scholar]
  89. Alasmary F. Snelling A. Zain M. Alafeefy A. Awaad A. Karodia N. Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents. Molecules 2015 20 8 15206 15223 10.3390/molecules200815206 26307956
    [Google Scholar]
  90. Alam S.A.M.F. Ahmad T. Nazmuzzaman M. Ray S.K. Ahammed T. Alam M.G. Sharifuzzaman M. Karim M.R. Ajam M. Maitra P. Mandol D. Uddin M.E. Synthesis of benzimidazole derivatives containing Schiff base exhibiting antimicrobial activities. Int. J. Res. Stud. Biosci. 2017 5 7 10.20431/2349‑0365.0507003
    [Google Scholar]
  91. Mohi A. Synthesis, theoretical and antimicrobial activity study of new benzimidazole derivatives. Egypt. J. Chem. 2020 63 8 2877 10.21608/ejchem.2020.21324.2272
    [Google Scholar]
  92. El-masry A.H. Fahmy H.H. Ali Abdelwahed S.H. Synthesis and antimicrobial activity of some new benzimidazole derivatives. Molecules 2000 5 12 1429 1438 10.3390/51201429
    [Google Scholar]
  93. Puratchikody A. Nagalakshmi G. Doble M. Experimental and QSAR studies on antimicrobial activity of benzimidazole derivatives. Chem. Pharm. Bull. 2008 56 3 273 281 10.1248/cpb.56.273 18310935
    [Google Scholar]
  94. Kuarm B.S. Madhav J.V. Rajitha B. ChemInform abstract: Synthesis and antimicrobial studies of selenadiazolo benzimidazoles. ChemInform 2014 45 18 chin.201418202 10.1002/chin.201418202
    [Google Scholar]
  95. Celik I. Çevik U.A. Karayel A. Işık A. Kayış U. Gül Ü.D. Bostancı H.E. Konca S.F. Özkay Y. Kaplancıklı Z.A. Synthesis, molecular docking, dynamics, quantum-chemical computation, and antimicrobial activity studies of some new benzimidazole-thiadiazole hybrids. ACS Omega 2022 7 50 47015 47030 10.1021/acsomega.2c06142 36570216
    [Google Scholar]
  96. Işık A. Acar Çevik U. Karayel A. Ahmad I. Patel H. Çelik İ. Gül Ü.D. Bayazıt G. Bostancı H.E. Koçak A. Özkay Y. Kaplancıklı Z.A. Synthesis, DFT calculations, in silico studies, and antimicrobial evaluation of benzimidazole-thiadiazole derivatives. ACS Omega 2024 9 16 18469 18479 10.1021/acsomega.4c00543 38680334
    [Google Scholar]
  97. Rostami H. Haddadi M.H. Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori-related diseases. Fundam. Clin. Pharmacol. 2022 36 6 930 943 10.1111/fcp.12810 35716372
    [Google Scholar]
  98. Noor A. Qazi N.G. Nadeem H. Khan A. Paracha R.Z. Ali F. Saeed A. Synthesis, characterization, anti-ulcer action and molecular docking evaluation of novel benzimidazole-pyrazole hybrids. Chem. Cent. J. 2017 11 1 85 10.1186/s13065‑017‑0314‑0 29086868
    [Google Scholar]
  99. Ayyad R. Sakr H.M. El-Gamal K.M. Eissa I. Tita A. Abd El-Raheim A.S. Sherbini F.F. Mansour A.M. Anti-inflammatory, proton pump inhibitor and synthesis of some NewBenzimidazole derivatives. Der Chemica Sinica 2017 8 1 168 181
    [Google Scholar]
  100. Wang M. Zhang C. Zhang Z. Xu X. He Y. Hu Y. Wang Y. Liu Y. Xia M. Cheng M. Discovery of novel benzimidazole derivatives as potent potassium-competitive acid blockers for the treatment of acid-related diseases. Bioorg. Chem. 2023 137 106588 10.1016/j.bioorg.2023.106588 37167705
    [Google Scholar]
  101. Taha M. Rahim F. Adalath B. Imran S. Mohammed Khan K. Adnan Ali shah, S.; Uddin, N.; Nawaz, M.; Break, M.K.B.; Magam, S.M.; Alqarni, S. Synthesis of benzimidazole derivatives and their antiglycation, antioxidant, antiurease and molecular docking study. Arab. J. Chem. 2024 17 4 105700 10.1016/j.arabjc.2024.105700
    [Google Scholar]
  102. Khan M.T. Razi M.T. Jan S.U. Mukhtiar M. Gul R. IzharUllah; Hussain, A.; Hashmi, A.M.; Ahmad, M.T.; Shahwani, N.A.; Rabbani, I. Synthesis, characterization and antihypertensive activity of 2-phenyl substituted benzimidazoles. Pak. J. Pharm. Sci. 2018 31 Suppl. 3 1067 1074 29731445
    [Google Scholar]
  103. Sethy S. Mandal S. Ewies E. Dhiman N. Garg A. Synthesis, characterization and biological evaluation of benzimidazole and benzindazole derivatives as anti-hypertensive agents. Egypt. J. Chem. 2021 64 3659 10.21608/ejchem.2021.79840.3931
    [Google Scholar]
  104. Wu Z. Xia M.B. Bertsetseg D. Wang Y.H. Bao X.L. Zhu W.B. Tao-Xu; Chen, P.R.; Tang, H.S.; Yan, Y.J.; Chen, Z.L. Design, synthesis and biological evaluation of novel fluoro-substituted benzimidazole derivatives with anti-hypertension activities. Bioorg. Chem. 2020 101 104042 10.1016/j.bioorg.2020.104042 32650179
    [Google Scholar]
  105. Han X.F. He X. Wang M. Xu D. Hao L.P. Liang A.H. Zhang J. Zhou Z.M. Discovery of novel, potent and low-toxicity angiotensin II receptor type 1 (AT1) blockers: Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazoles with a chiral center. Eur. J. Med. Chem. 2015 103 473 487 10.1016/j.ejmech.2015.09.010 26397395
    [Google Scholar]
  106. Zhang Y. Xu J. Li Y. Yao H. Wu X. Design, synthesis and pharmacological evaluation of novel NO-releasing benzimidazole hybrids as potential antihypertensive candidate. Chem. Biol. Drug Des. 2015 85 5 541 548 10.1111/cbdd.12442 25283264
    [Google Scholar]
  107. Bharadwaj S.S. Poojary B. Nandish S.K.M. Kengaiah J. Kirana M.P. Shankar M.K. Das A.J. Kulal A. Sannaningaiah D. 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 2018 3 10 12562 12574 10.1021/acsomega.8b01476 30411010
    [Google Scholar]
  108. Arora M. Microwave-assisted synthesis, characterization, computational studies and in-vitro anthelmintic, antioxidant and anticoagulant activities of some novel benzimidazoles. Afr J. Bio Sci. 2024 6 10 4945 4959 10.48047/AFJBS.6.10.2024.4945‑4959
    [Google Scholar]
  109. Argirova M.A. Georgieva M.K. Hristova-Avakumova N.G. Vuchev D.I. Popova-Daskalova G.V. Anichina K.K. Yancheva D.Y. New 1 H -benzimidazole-2-yl hydrazones with combined antiparasitic and antioxidant activity. RSC Advances 2021 11 63 39848 39868 10.1039/D1RA07419A 35494105
    [Google Scholar]
  110. Bhandari S.V. Nagras O.G. Kuthe P.V. Sarkate A.P. Waghamare K.S. Pansare D.N. Chaudhari S.Y. Mawale S.N. Belwate M.C. Design, synthesis, molecular docking and antioxidant evaluation of benzimidazole-1,3,4 oxadiazole derivatives. J. Mol. Struct. 2023 1276 134747 10.1016/j.molstruc.2022.134747
    [Google Scholar]
  111. Aroua L.M. Alosaimi A.H. Alminderej F.M. Messaoudi S. Mohammed H.A. Almahmoud S.A. Chigurupati S. Albadri A.E.A.E. Mekni N.H. Synthesis, molecular docking, and bioactivity study of novel hybrid benzimidazole urea derivatives: A promising α-amylase and α-glucosidase inhibitor candidate with antioxidant activity. Pharmaceutics 2023 15 2 457 10.3390/pharmaceutics15020457 36839780
    [Google Scholar]
/content/journals/ctmc/10.2174/0115680266425342260112130801
Loading
Exploring the Pharmacological Profiles of Benzimidazole Derivatives: A Comprehensive Review
Bentham Science Publishers ; https://doi.org/10.2174/0115680266425342260112130801
/content/journals/ctmc/10.2174/0115680266425342260112130801
/content/journals/ctmc/10.2174/0115680266425342260112130801
Loading

Data & Media loading...


  • Article Type:     Review Article
Keywords: Fused heterocyclic scaffolds ; Bioactive compounds ; Benzimidazole ; Therapeutic applications ; Molecular docking ; Structure–activity relationship

Most Cited Most Cited RSS feed

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test