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Journal articles on the topic 'Benzimidazoles'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Al-Warhi, Tarfah, Mohamed Said, Mahmoud El Hassab, et al. "Unexpected Synthesis, Single-Crystal X-ray Structure, Anticancer Activity, and Molecular Docking Studies of Certain 2–((Imidazole/Benzimidazol–2–yl)thio)–1–arylethanones." Crystals 10, no. 6 (2020): 446. http://dx.doi.org/10.3390/cryst10060446.

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In connection with our research program concerning development of novel effective benzimidazole-based anticancer candidates, herein we describe a new unexpected synthetic route to obtain a series of 2–((imidazole/benzimidazol2–yl)thio)1–arylethanones endowed with promising anti-breast cancer and Cyclin-dependent kinase 2 (CDK2) inhibitory activities. Contrary to expectations, products for the reaction of 2–mercaptoimidazole/benzimidazole 2a,b with β–keto esters 6a–c were unambiguously assigned as 2–((imidazol/benzimidazol2–yl)thio)1–arylethanones 10a–f based on NMR spectroscopy and single-crys

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2

Krishnamurthy, Naik, and Narashimaiah Shashikala. "Synthesis of ruthenium(II) carbonyl complexes with 2-monosubstituted and 1,2-disubstituted benzimidazoles." Journal of the Serbian Chemical Society 74, no. 10 (2009): 1085–96. http://dx.doi.org/10.2298/jsc0910085k.

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The reaction of the polymeric carbonyl complex [RuCl2(CO)2]x with 2-monosubstituted and 1,2-disubstituted benzimidazoles and 1,4-bis(benzimidazol- 2-yl)benzene (L9) in 2-methoxyethanol produces various coloured complexes of the formulae [Ru(CO)2Cl2(L)2]?xH2O (L = 1-(o-hydroxybenzyl)-2-(o-hydroxyphenyl)benzimidazole (L1), 1-(o-hydroxyphenyl)benzimidazole (L4), 1-(p-hydroxyphenyl)benzimidazole (L5), 1-(p-chlorobenzyl)-2-p-chlorophenyl) benzimidazole (L7), 1-[1-(dimethylamino)benzyl]-2-[1-(dimethylamino) phenyl]benzimidazole (L10), x = 0; L = 2-benzylbenzimidazole (L8), 1,4-bis(benzimidazol-2-yl)

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3

Padhy, Gopal Krishna, Jagadeesh Panda, Chandra Sekhar Patr, Saroj Kumar Raul, and Ajaya Kumar Behera. "SYNTHETIC APPROACHES OF BENZIMIDAZOLE DERIVATIVES: A REVIEW." RASAYAN Journal of Chemistry 16, no. 04 (2023): 2009–18. http://dx.doi.org/10.31788/rjc.2023.1648014.

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Benzimidazole is considered a privileged moiety for the development of molecules with therapeutic potential. Over the years several drugs viz: albendazole, pantoprazole, astemizole, telmisartan, thiabendazole, and benomyl have been developed by optimizing benzimidazole-based structures. Given the various pharmacological implications of benzimidazoles, it encourages to explore new synthetic protocols for benzimidazoles. The review presented here highlights exclusively the recent synthetic approaches to prepare benzimidazole derivatives. Numerous search engines like Science Direct, Semantic Scho

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4

Kumawat, Deepak, and Harshal Tare. "Benzimidazoles in Medicinal Chemistry: Current Trends and Future Opportunities." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 15, no. 01 (2024): 554–61. http://dx.doi.org/10.25258/ijpqa.15.1.83.

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Because of their various pharmacological actions and structural plasticity, benzimidazoles, a class of heterocyclic molecules, have received much attention in medicinal chemistry. This review paper aims to provide a complete overview of the current developments and future possibilities of benzimidazoles as promising candidates for the creation of innovative therapeutic medicines. The introduction discusses the importance of benzimidazoles in medicinal chemistry, emphasizing their wide range of uses, which include antibacterial, anticancer, and central nervous system actions. The structural pro

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5

Song, Bomi, Eun Young Park, Kwang Joon Kim, and Sung Hwan Ki. "Repurposing of Benzimidazole Anthelmintic Drugs as Cancer Therapeutics." Cancers 14, no. 19 (2022): 4601. http://dx.doi.org/10.3390/cancers14194601.

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Benzimidazoles have shown significant promise for repurposing as a cancer therapy. The aims of this review are to investigate the possibilities and limitations of the anti-cancer effects of benzimidazole anthelmintics and to suggest ways to overcome these limitations. This review included studies on the anti-cancer effects of 11 benzimidazoles. Largely divided into three parts, i.e., preclinical anti-cancer effects, clinical anti-cancer effects, and pharmacokinetic properties, we examine the characteristics of each benzimidazole and attempt to elucidate its key properties. Although many studie

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6

Kumar, Sushil, Maneesha D. Sati, and S. C. Sati. "Synthesis And Biological Evaluation Of Benzimidazole Derivatives." IOSR Journal of Applied Chemistry 17, no. 12 (2024): 13–18. https://doi.org/10.9790/5736-1712011318.

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Benzimidazoles are a class of heterocyclic compounds in which a benzene ring is fused to the 4 and 5 positions of an imidazole ring. Benzimidazole refers to the parent compound, while benzimidazoles are a class of heterocyclic compounds having similar ring structures, but different substituents. Benzimidazole derivatives possess a wide range of bioactivities including antimicrobial, anthelmintic, antiviral, anticancer, and antihypertensive activities. Many compounds possessing a benzimidazole skeleton have been employed as drugs in the market. The application of benzimidazoles in other fields

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7

Hajnal, Kelemen, Mărcuțiu Petra Edina, Rausz Adrienn, and Papp Lajos-Attila. "Chemical and pharmacological characterization of anthelmintic benzimidazoles." Bulletin of Medical Sciences 94, no. 2 (2021): 88–96. http://dx.doi.org/10.2478/orvtudert-2021-0013.

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Abstract Benzimidazoles, which interfere with the complex life cycle of worms, are essential in the treatment of helminthiasis. Four benzimidazole antihelmintics have been used in human therapy: albendazole, mebendazole, thiabendazole, triclabendazole. The history, representatives, synthesis, physicochemical properties, structure-activity relationships of anthelmintic benzimidazoles are presented in the review, as well as the pharmacological properties and mechanism of action of these agents. In the last decade, benzimidazole carbamate-structured anthelmintics have also been studied for their

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8

Wang, Cheng Jun, De Yun Zeng, Shan Shan Gong, and Qi Sun. "An Unexpected Synthesis of 2H-Benzimidazole Derivatives." Advanced Materials Research 1023 (August 2014): 43–46. http://dx.doi.org/10.4028/www.scientific.net/amr.1023.43.

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Treatment of 1,2-phenylenediamines and 3-(N-phenyl-N-methyl) aminoacrolein with ZrCl4as catalyst in refluxing 95% ethanol afforded unexpected 2H-benzimidazole derivatives as the major products. It was determined that the formation of 2H-benzimidazoles was not from the decomposition of the 2-aminovinyl benzimidazoles.

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9

Bektas, Hakan, Canan Albay, Emre Menteşe, Bahar Bilgin Sokmen, Zafer Kurt, and Dilem Şen. "Synthesis, Antioxidant and Antiurease Activities of Some New 5,6- dichloro-2-(4-fluorobenzyl)-1H-benzimidazole Derivatives Containing Furan, Oxadiazole, Triazole and Thiadiazole Moieties." Letters in Drug Design & Discovery 16, no. 8 (2019): 939–47. http://dx.doi.org/10.2174/1570180815666180827124956.

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Background:Benzimidazoles and its derivatives have been attracting interest for many years because of their biological activities. Benzimidazoles containing different heterocyclic moieties have wide range of biological activities such as antimicrobial, antioxidant, anticancer, antiviral, etc.Methods:In this study, some benzimidazole derivatives containing furan, oxadiazole, triazole and thiadiazole moieties have been synthesized and then evaluated for their antioxidant and antiurease activities.Results:The results showed that all the tested benzimidazoles indicated remarkable urease inhibitory

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10

Nardi, Monica, Sonia Bonacci, Natividad Herrera Cano, Manuela Oliverio, and Antonio Procopio. "The Highly Efficient Synthesis of 1,2-Disubstituted Benzimidazoles Using Microwave Irradiation." Molecules 27, no. 5 (2022): 1751. http://dx.doi.org/10.3390/molecules27051751.

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The benzimidazole ring of the heterocyclic pharmacophores is one of the most widespread and studied systems in nature. The benzimidazole derivative synthesis study is a crucial point for the development of a clinically available benzimidazole-based drug. Here, we report a simple microwave assisted method for the synthesis of 1,2-disubstituted benzimidazoles. The combination of the molar ratio of N-phenyl-o-phenylenediamine:benzaldehyde (1:1) using microwave irradiation and only 1% mol of Er(OTf)3 provides an efficient and environmental mild access to a diversity of benzimidazoles under solvent

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11

Begunov, Roman S., and Alexandr A. Sokolov. "SYNTHESIS AND MASS SPECTROMETRIC CHARACTERISTICS OF 1-(AMINOARYL)BENZIMIDAZOLES." IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENII KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 63, no. 9 (2020): 12–20. http://dx.doi.org/10.6060/ivkkt.20206309.6230.

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As a result of two-stage synthesis, a number of 1-(aminoaryl)benzimidazoles, potential biologically active substances, were obtained. During the first stage, an aromatic nucleophilic substitution reaction, 2-R-benzimidazoles reacted with halogen-nitroarenes. The process proceeded under mild conditions, this indicates a good nucleophilic properties of benzimidazole. It has been shown that during reduction, depending on the structure of 1-(nitroaryl)benzimidazoles in an acidic medium, in addition to the main process, acid-catalyzed isomerization can occur. Rearrangement was observed during the r

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12

Andric, Deana, Gordana Tovilovic, Goran Roglic, et al. "Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives." Journal of the Serbian Chemical Society 72, no. 5 (2007): 429–35. http://dx.doi.org/10.2298/jsc0705429a.

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Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, expressed higher affinities for all receptor classes than clozapi

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13

Barasa, Leonard, Hari P. Vemana, Nirupama Surubhotla, et al. "Synthesis and Biological Evaluation of Structurally Diverse Benzimidazole Scaffolds as Potential Chemotherapeutic Agents." Anti-Cancer Agents in Medicinal Chemistry 20, no. 3 (2020): 301–14. http://dx.doi.org/10.2174/1871520619666191028101506.

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Background and Objective : Drug resistance and adverse effects are immense healthcare challenges in cancer therapy. Benzimidazole ring-based small molecules have been effective anticancer agents in drug development. In an effort to develop novel chemotherapeutics, we synthesized and assessed the anticancer and antibacterial activities of a small library of structurally unique benzimidazoles. Methods : The benzimidazoles were derived from indole, N-alkyl indole, fatty acid, and alpha-amino acid scaffolds providing a panel of diverse structures. The compounds were tested in three different cance

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14

Monika*, Ramanpreet Kaur Ravinder Sharma Gunpreet Kaur Harjinder Singh. "SYNTHESIS AND ANTIMICROBIAL ACTIVITIES OF NOVEL BENZIMIDAZOLE DERIVATIVES." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 01 (2018): 706–11. https://doi.org/10.5281/zenodo.1174182.

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<em>Benzimidazole </em><em>is a heterocyclic aromatic organic compound. Benzimidazole derivatives are of wide interest because of their diverse biological activity and clinical applications, they are remarkably effective compounds both with respect to their inhibitory activity and their favorable selectivity ratio. Looking at the importance of benzimidazole and oxadiazole nucleus, it was thought that it would be worthwhile to design and synthesize new benzimidazole derivatives. In recent years, attention has increasingly been given to the synthesis of benzimidazole derivatives. Hence, there wi

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15

Goossens, Laurence, Omar Castillo-Aguilera, Patrick Depreux, Alexia Ballée, Florian Beaurain, and Paola B. Arimondo. "Study of the Effect of Substituents of ortho-Phenylenediamines in the Opening of Lactones and Lactams for Access to Benzimidazol-2-yl Alkanols and Benzimidazol-2-yl Alkylamines." Synlett 31, no. 12 (2020): 1216–20. http://dx.doi.org/10.1055/s-0040-1707112.

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Benzimidazoles represent common chemical moieties in bioactive compounds. The synthesis of this heterocycle often involves a condensation of an ortho-phenylenediamine with a carboxylic acid derivative. The observed dialkylation of the starting ortho-phenylenediamine is avoided by opening of lactones or lactams. This strategy can directly yield 1H-benzimidazoles substituted at the 2-position by a functionalized chain. We present herein a study of the effect of different electron-withdrawing or electron-donating groups at the 4-position of ortho-phenylenediamines on the opening of lactones or la

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16

Chung, Nguyen Thi, Vo Cong Dung, and Dau Xuan Duc. "Recent achievements in the synthesis of benzimidazole derivatives." RSC Advances 13, no. 46 (2023): 32734–71. http://dx.doi.org/10.1039/d3ra05960j.

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This article gives a comprehensive review on the synthesis of benzimidazoles including reaction mechanisms and a brief description of biological application of benzimidazole derivatives by summarizing recent studies.

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17

Nieto, Carla I., Pilar Cabildo, M. Ángeles García, Rosa M. Claramunt, Ibon Alkorta, and José Elguero. "An experimental and theoretical NMR study of NH-benzimidazoles in solution and in the solid state: proton transfer and tautomerism." Beilstein Journal of Organic Chemistry 10 (July 16, 2014): 1620–29. http://dx.doi.org/10.3762/bjoc.10.168.

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This paper reports the 1H, 13C and 15N NMR experimental study of five benzimidazoles in solution and in the solid state (13C and 15N CPMAS NMR) as well as the theoretically calculated (GIAO/DFT) chemical shifts. We have assigned unambiguously the "tautomeric positions" (C3a/C7a, C4/C7 and C5/C6) of NH-benzimidazoles that, in some solvents and in the solid state, appear different (blocked tautomerism). In the case of 1H-benzimidazole itself we have measured the prototropic rate in HMPA-d 18.

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18

Bansal, Yogita, Manjinder Kaur, and Gulshan Bansal. "Antimicrobial Potential of Benzimidazole Derived Molecules." Mini-Reviews in Medicinal Chemistry 19, no. 8 (2019): 624–46. http://dx.doi.org/10.2174/1389557517666171101104024.

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Structural resemblance of benzimidazole nucleus with purine nucleus in nucleotides makes benzimidazole derivatives attractive ligands to interact with biopolymers of a living system. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. This structural similarity prompted medicinal chemists across the globe to synthesize a variety of benzimidazole derivatives and to screen those for various biological activities, such as anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, a

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19

Sweeney, Martin, Darren Conboy, Styliana I. Mirallai, and Fawaz Aldabbagh. "Advances in the Synthesis of Ring-Fused Benzimidazoles and Imidazobenzimidazoles." Molecules 26, no. 9 (2021): 2684. http://dx.doi.org/10.3390/molecules26092684.

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This review article provides a perspective on the synthesis of alicyclic and heterocyclic ring-fused benzimidazoles, imidazo[4,5-f]benzimidazoles, and imidazo[5,4-f]benzimidazoles. These heterocycles have a plethora of biological activities with the iminoquinone and quinone derivatives displaying potent bioreductive antitumor activity. Synthesis is categorized according to the cyclization reaction and mechanisms are detailed. Nitrobenzene reduction, cyclization of aryl amidines, lactams and isothiocyanates are described. Protocols include condensation, cross-dehydrogenative coupling with trans

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20

Long, Austin R., Lily C. Hsieh, Marsha S. Malbrough, Charles R. Short, and Steven A. Barker. "Multiresidue Method for Isolation and Liquid Chromatographic Determination of Seven Benzimidazole Anthelmintics in Milk." Journal of AOAC INTERNATIONAL 72, no. 5 (1989): 739–41. http://dx.doi.org/10.1093/jaoac/72.5.739.

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Abstract A multiresidue method for the isolation and liquid chromatographic determination of 7 benzimidazole anthelmintics (thiabendazole, oxfendazole, para-hydroxyfenbendazole, fenbendazole sulfone, mebendazole, albendazole, and fenbendazole) in milk is presented. Blank or benzimidazole-spiked milk samples (0.5 mL) were blended with octadecylsilyl (C-18, 18% load, end-capped) derivatized silica packing material. A column made from the C-18/milk matrix was first washed with hexane (8 mL), and then the benzimidazoles were eluted with methylene chloride-ethyl acetate (1 + 2, v/v; 8 mL). The elua

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21

G., C. KAMDAR, J. BHATT D. та R. PARIKH A. "Studies on Benzimidazole. Preparation and Antimicrobial Activity of 2-(α-Arylaminobenzyl)benzimidazoles and 2-(2',3'-Diaryl-4'- keto-5'-thiazolidinyl)methylbenzimidazoles". Journal of Indian Chemical Society Vol. 65, Jan 1988 (1988): 67–68. https://doi.org/10.5281/zenodo.6122482.

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Department of Chemistry, Saurashtra University, Rajkot-360 005 <em>Manuscript received 16 June 1983,revised 2 November 1987, accepted 13 November 1987</em> Studies on Benzimidazole. Preparation and Antimicrobial Activity of 2-(α-Arylaminobenzyl)benzimidazoles and 2-(2',3'-Diaryl-4'- keto-5'-thiazolidinyl)methylbenzimidazoles.

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22

Vasantha T S, Shankar Mani, T. Yunus Pasha, and B. Ramesh. "A comprehensive review on 2-substituted benzimidazole derivatives and its biological importance." International Journal of Scholarly Research and Reviews 2, no. 2 (2023): 122–34. http://dx.doi.org/10.56781/ijsrr.2023.2.2.0032.

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Condensation of o-phenylene-diamine with formic acid is used in the synthesis of commercially available benzimidazole. N-ribosyldimethyl benzimidazole is the most common benzimidazole compound found in nature, and it functions as an axial ligand for cobalt in vitamin B12. The benzimidazole and its derivatives are important therapeutic agents, such as antiulcer and anthelmintic drugs. Benzimidazole compounds also possess antimicrobial, antiviral, anticancer, anti-inflammatory, analgesic, and other pharmacological properties. The chemistry and pharmacological actions of substituted benzimidazole

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23

A., K. SINHA, URMILA KUMARI (Mrs.), P. SINGH C., and K. MISHRA L. "Oxovanadium(IV) Complexes with Imidazole, Benzimidazole and Substituted Benzimidazoles." Journal Of Indian Chemical Society Vol. 67, Dec 1990 (1990): 985–86. https://doi.org/10.5281/zenodo.6275154.

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Department of Chemistry. Patna University. Patna-800 005 <em>Manuscript received 1 November 1989, revised 15 October 1990, accepted 6 November 1990</em> Oxovanadium(IV) Complexes with Imidazole, Benzimidazole and Substituted Benzimidazoles

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24

Yadrova, Anastasia A., Roman V. Shafigulin, and Andzhela V. Bulanova. "Study the effect of eluent composition on benzimidazole and its derivatives retention on hypercrosslinked polystyrene." Butlerov Communications 58, no. 5 (2019): 75–80. http://dx.doi.org/10.37952/roi-jbc-01/19-58-5-75.

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The effect of water-acetonitrile and water-methanol eluents composition on newly synthesized benzimidazole derivatives sorption by supercrosslinked polystyrene (SCP) using high performance liquid chromatography was studied. It is shown that the nature of the organic modifier affects on the considered biologically active compounds sorption. The angular coefficients of the Snyder-Sochevinsky equation, characterizing the number of organic modifier molecules, displaced by one molecule of sorbate, for benzimidazole derivatives, are calculated. The angular coefficients was calculated from the depend

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25

Jalil, Nurul Awani Syazzira, and Shafida Abd Hamid. "Molecular Docking Analysis on the Designed Benzimidazole Derivatives as EGFR Inhibitors: Comparison between EGFR Wild-Type (EGFRWT) and T790M Mutant." Sains Malaysiana 52, no. 4 (2023): 1203–15. http://dx.doi.org/10.17576/jsm-2023-5204-13.

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The non-small cell lung (NSCL) and colorectal cancers are frequently linked with the oncogenic activation of the epidermal growth factor receptor (EGFR), a member of the receptor tyrosine kinase (RTK) family. Current tyrosine kinase inhibitors (TKIs) are susceptible to drug resistance mutations and induce cytotoxicity effects on normal EGFRs. The isosteric nature of benzimidazole with purine renders its great potential to imitate the binding mode of the purine-based ATP and prevents its contact with the EGFR active sites. Here, we report the molecular docking of 50 designed benzimidazole deriv

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26

Xu, Zhigang, Arthur Y. Shaw, Justin Dietrich, Alexandra P. Cappelli, Gary Nichol, and Christopher Hulme. "Facile, novel two-step syntheses of benzimidazoles, bis-benzimidazoles, and bis-benzimidazole-dihydroquinoxalines." Molecular Diversity 16, no. 1 (2012): 73–79. http://dx.doi.org/10.1007/s11030-011-9354-x.

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27

Ibrahim, Hassan K., Sayed H. El-Tamany, Reda F. El-Shaarawy, and Ibrahim M. El-Deen. "Synthesis and investigation of mass spectra of some novel benzimidazole derivatives." Macedonian Journal of Chemistry and Chemical Engineering 27, no. 1 (2008): 65. http://dx.doi.org/10.20450/mjcce.2008.248.

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2-Substituted benzimidazoles (3) and (4a-c) were prepared via condensation of ethyl 2-thionyl-pyruvate (1) and hydrazidoyl derivatives (2a-c) with o-phenylene diamine in acetic acid. Acetylation of compound (4a) with acetic anhydride yielded the corresponding N-acetyl derivative (5). Treatment of compound 4b with hydrazine hydrate gave the corresponding hydrazino derivative (6). Reaction of 2-[(2-thionyl)acetyl)] benzimidazole (3) with hydrazine hydrate gave the pyrazolyl derivative (7) and hydrazino derivative (8). Alkylation of compound 3 with alkyl halide gave the corresponding 2,3-disubsti

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Sachin S. Kale. "Densities and Apparent Molar Volume of Benzimidazole in Pure and Binary Solvent Mixtures of Ethanol + Water." International Journal of Scientific Research in Science and Technology 11, no. 4 (2024): 356–61. http://dx.doi.org/10.32628/ijsrst24114133.

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Benzimidazole is an important pharmacophore in medicinal chemistry. Benzimidazoles are having a many therapeutic uses like antibacterial, antifungal, analgesics, antitumor, antiparasitic, antihistamine, and antiviral. Using bicapillary pycnometer densities of Benzimidazole in ethanol with water were measured over the entire composition range at temperatures from 293.15 to 313.15 K. Densities of the saturated solution of benzimidazole in a pure and binary mixture of solvents were measured at mentioned temperature. This density data was used to calculate apparent molar volume. The apparent molar

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Šoškić, V., and Jelena Joksimović. "Bioisosteric Approach In The Design of New Dopaminergic/ Serotonergic Ligands." Current Medicinal Chemistry 5, no. 6 (1998): 493–512. http://dx.doi.org/10.2174/0929867305666220319113953.

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Dopaminergic and serotonergic ligands are widely applied in the therapy of some severe diseases in humans connected to the malfunctioning of the corresponding membrane receptors within the CNS. However, no pharmaceuticals of this type with an ideal therapeutic index have been synthesized so far and there is a constant need of producing new dopaminergic/serotonergic ligands with improved properties especially with regard to undesirable side effects expressed after a prolonged therapy. Dopaminergic/serotonergic ratio turned out to be important for a fine tuning of pharmacological profile of new

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Veerasamy, Ravichandran, Anitha Roy, Rohini Karunakaran, and Harish Rajak. "Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview." Pharmaceuticals 14, no. 7 (2021): 663. http://dx.doi.org/10.3390/ph14070663.

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A significant number of the anti-inflammatory drugs currently in use are becoming obsolete. These are exceptionally hazardous for long-term use because of their possible unfavourable impacts. Subsequently, in the ebb-and-flow decade, analysts and researchers are engaged in developing new anti-inflammatory drugs, and many such agents are in the later phases of clinical trials. Molecules with heterocyclic nuclei are similar to various natural antecedents, thus acquiring immense consideration from scientific experts and researchers. The arguably most adaptable heterocyclic cores are benzimidazole

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Francesconi, Valeria, Elena Cichero, Silvia Schenone, Lieve Naesens, and Michele Tonelli. "Synthesis and Biological Evaluation of Novel (thio)semicarbazone-Based Benzimidazoles as Antiviral Agents against Human Respiratory Viruses." Molecules 25, no. 7 (2020): 1487. http://dx.doi.org/10.3390/molecules25071487.

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Respiratory RNA viruses are responsible for recurrent acute respiratory illnesses that still represent a major medical need. Previously we developed a large variety of benzimidazole derivatives able to inhibit these viruses. Herein, two series of (thio)semicarbazone- and hydrazone-based benzimidazoles have been explored, by derivatizing 5-acetyl benzimidazoles previously reported by us, thereby evaluating the influence of the modification on the antiviral activity. Compounds 6, 8, 16 and 17, bearing the 5-(thio)semicarbazone and 5-hydrazone functionalities in combination with the 2-benzyl ring

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Abdullah, Asmaa M., Abdull Jabar Kh Attia, and Sergei N. Shtykov. "Synthesis and Characterization of Novel Benzimidazole Derivatives using CdO NPs and their Application as Antibacterial and Antifungal Agents." Al-Mustansiriyah Journal of Science 35, no. 4 (2024): 52–63. https://doi.org/10.23851/mjs.v35i4.1572.

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Background: Benzimidazoles are a class of compounds characterized by a fusion of benzene and imidazole rings. This unique structure endows them with a broad spectrum of biological activities, making them invaluable in medicinal and pharmaceutical research. The benzene ring provides aromatic stability, while the imidazole ring offers a site for various chemical modifications, enhancing their versatility and functionality. Benzimidazoles are known for their diverse pharmacological properties, including antimicrobial, antiviral, anticancer, anti-inflammatory, and antiparasitic. Objective: Synthes

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Sochnev, V. S., Yu V. Koshchienko, T. A. Kuz'menko, A. A. Kolodina, G. S. Borodkin, and A. S. Morkovnik. "Bromination of 1(9)<i>H</i>-2,3-dihydroimidazo[1,2-<i>a</i>]benzimidazole and its <i>N</i>-derivatives." Журнал общей химии 93, no. 6 (2023): 858–66. http://dx.doi.org/10.31857/s0044460x23060045.

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2,3-Dihydro-1 H -imidazo[1,2- a ]benzimidazole in acetic acid, and its N 1-Me derivative in CHCl3, are brominated at position 6 with bromine. Less nucleophilic N 9-R derivatives do not enter into the reaction under these conditions, but, like their N 1-R isomers, they are quite effectively brominated by the KBrO3-HBr system, but at position 7, probably due to the transition of the reaction to the mode of bromination of protonated forms of substrates. N 1- and N 9-alkyl-6(7)-Br-2,3-dihydroimidazo[1,2- a ]benzimidazoles can also be obtained by N -alkylation of 6(7)-Br-2,3-dihydroimidazo[1,2- a ]

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34

Babbar, Ritchu, Swikriti ., Sandeep Arora, and Thakur G. Singh. "Therapeutic Potential of Schiff and Mannich Bases of 2-Substituted Benzimidazole Analogues." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 13, no. 02 (2022): 753–58. http://dx.doi.org/10.25258/ijddt.13.2.44.

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Heterocyclic scaffolds reveal extensive biological profiles, and several drugs were employed therapeutically which possess heterocyclic framework. Likewise, 2-substituted benzimidazoles play a significant role in novel drug development. In addition, Mannich and schiff base derivatives of benzimidazole acknowledged them as favorable anti-inflammatory, antimicrobial, anticancer, anthelmintic, antiviral scaffolds. Schiff bases in innumerable organic reactions show affirmative catalytic activity. The current scenario also emphasizes the spectacular activity displayed by schiff bases in the biochem

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35

Autier, Brice, Florence Robert-Gangneux, and Sarah Dion. "Chemotherapy for the treatment of alveolar echinococcosis: Where are we?" Parasite 31 (2024): 56. http://dx.doi.org/10.1051/parasite/2024055.

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Alveolar echinococcosis (AE) is a severe liver disease due to infection with the Echinococcus multilocularis larval stage, called the metacestode. Management of AE is based on benzimidazole chemotherapy (albendazole or mebendazole), associated with surgery when possible. Benzimidazoles are the only compounds recommended for the treatment of AE; however, these are parasitostatic, which means that the parasite can resume growth when treatment is interrupted. Also, benzimidazoles can cause liver dysfunction which may prevent their use. Numerous drugs have been reported to have in vitro activity a

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36

Janani, Marzieh, Masumeh Abdoli Senejani, and Tahereh Momeni Isfahani. "An Efficient Synthesis of Benzimidazole and Benzothiazole Derivatives Using a Nickel(II) Metal-Organic Framework." Current Organic Synthesis 17, no. 2 (2020): 109–16. http://dx.doi.org/10.2174/1570179417666200117110758.

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Background: The benzimidazoles and benzothiazoles have shown relatively high pharmaceutical and biological activities. In recent years, numerous methods have been developed for synthesis of benzimidazole and benzothiazole derivatives using different catalysts. However, only some of the reported procedures are quite satisfactory and most of them have drawbacks. Herein, we report a convenient method for synthesis of benzimidazole and benzothiazole derivatives using a nickel (II) metal-organic framework (Ni- MOF) as a novel and reusable catalyst. The presence of unsaturated metal centers makes me

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Xu, Zhigang, Arthur Y. Shaw, Justin Dietrich, Alexandra P. Cappelli, Gary Nichol, and Christopher Hulme. "ChemInform Abstract: Facile, Novel Two-Step Syntheses of Benzimidazoles, Bis-benzimidazoles, and Bis-benzimidazole-dihydroquinoxalines." ChemInform 43, no. 35 (2012): no. http://dx.doi.org/10.1002/chin.201235129.

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García-Báez, Efrén V., Itzia I. Padilla-Martínez, Alejandro Cruz, and Martha C. Rosales-Hernández. "13C-NMR Chemical Shifts in 1,3-Benzazoles as a Tautomeric Ratio Criterion." Molecules 27, no. 19 (2022): 6268. http://dx.doi.org/10.3390/molecules27196268.

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Benzimidazole is an important heterocyclic fragment, present in many biologically active compounds with a great variety of therapeutic purposes. Most of the benzimidazole activities are explained through the existence of 1,3-tautomeric equilibrium. As the binding affinity of each tautomer to a protein target depends on an established bioactive conformation, the effect of tautomers on the ligand protein binding mechanism is determinant. In this work, we searched and analyzed a series of reported 13C-NMR spectra of benzazoles and benzazolidine-2-thiones with the purpose of estimating their tauto

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39

Kazimierczuk, Zygmunt, Jacqueline A. Upcroft, Peter Upcroft, Agata Górska, Bohdan Starościak, and Agnieszka Laudy. "Synthesis, antiprotozoal and antibacterial activity of nitro- and halogeno-substituted benzimidazole derivatives." Acta Biochimica Polonica 49, no. 1 (2002): 185–95. http://dx.doi.org/10.18388/abp.2002_3835.

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Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia, and an activity comparable to that of metronidazole against gram-positive and gram-negative bacteria. Of the tested compounds, 5,6-dichloro-2-(4-nitrobenzylthio)-benzimidazole showed the most distinct

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Franzen, Caspar, та Bernd Salzberger. "Analysis of the β-Tubulin Gene from Vittaforma corneae Suggests Benzimidazole Resistance". Antimicrobial Agents and Chemotherapy 52, № 2 (2007): 790–93. http://dx.doi.org/10.1128/aac.00928-07.

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ABSTRACT We amplified, cloned, and sequenced the β-tubulin gene of Vittaforma corneae, a microsporidium causing human infections. The β-tubulin gene sequence has a substitution at Glu198 (with glutamine), which is one of six amino acids reported to be associated with benzimidazole sensitivity. Benzimidazoles were assayed for antimicrosporidial activity and showed poor parasite inhibition.

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Xie, Caixia, Xushuang Han, Jian Gong, Danyang Li, and Chen Ma. "One-pot strategy of copper-catalyzed synthesis of 1,2-disubstituted benzimidazoles." Organic & Biomolecular Chemistry 15, no. 27 (2017): 5811–19. http://dx.doi.org/10.1039/c7ob00945c.

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A simple, one-pot and copper-catalyzed coupling reaction for the construction of 1,2-disubstituted benzimidazole derivatives is described. A low-cost copper salt and a weak base, K<sub>3</sub>PO<sub>4</sub>, were utilized in this reaction. A variety of 1,2-disubstituted benzimidazoles were obtained in moderate to excellent yields.

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Hangarage, Rahul V., Bhushan B. Khairnar, Rajashree B. Sawant, Harshad R. Sonawane, Pravin N. Chavan, and Jaydeep V. Deore. "Synthetic of Benzimidazole analogs based on the O-phenylenediamine: A mini review." Current Chemistry Letters 14, no. 2 (2025): 323–38. https://doi.org/10.5267/j.ccl.2024.11.003.

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Heterocyclic molecules are found in many parts of living things, so they are being used more and more in medicinal chemistry. Benzimidazoles, which are naturally occurring compounds, exhibit a diverse array of pharmaceutical properties that have been extensively documented. Benzimidazole derivatives serve as valuable intermediates or subunits in the synthesis of pharmaceutical or biologically significant compounds. Substituted benzimidazole derivatives have been utilized in various therapeutic domains, encompassing but not limited to antiulcer, anticancer agents, and anthelmintic species. This

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Rao, S. Srinivas, Ch Venkata Ramana Reddy, and P. K. Dubey. "Synthesis of N-Alkyl-2-thiomethyl Benzimidazoles: A Green Approach." Organic Chemistry International 2014 (March 17, 2014): 1–4. http://dx.doi.org/10.1155/2014/239710.

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A green approach for the synthesis of N-alkyl-2-thiomethyl benzimidazoles 2 (R=CH3, C2H5, CH2Ph) under different conditions has been developed from N-alkyl-2-chloromethyl benzimidazole (i.e., CH3, C2H5, CH2Ph) 1 by reaction with thiourea by physical grinding, or by using green solvents like ethanol and PEG-600, or by using microwave irradiation technique.

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Sontakke, Vyankat A., Sougata Ghosh, Pravin P. Lawande, Balu A. Chopade, and Vaishali S. Shinde. "A Simple, Efficient Synthesis of 2-Aryl Benzimidazoles Using Silica Supported Periodic Acid Catalyst and Evaluation of Anticancer Activity." ISRN Organic Chemistry 2013 (April 24, 2013): 1–7. http://dx.doi.org/10.1155/2013/453682.

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A new, efficient method for the synthesis of 2-aryl substituted benzimidazole by using silica supported periodic acid (H5IO6-SiO2) as a catalyst has been developed. The salient feature of the present method includes mild reaction condition, short reaction time, high yield and easy workup procedure. The synthesized benzimidazoles exhibited potent anticancer activity against MCF7 and HL60 cell lines.

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45

Kapoor, Kamal, Parthasarathi Das, Rajni Khajuria, Sk Rasheed, and Chhavi Khajuria. "Recent Developments in the Synthesis of Pyrido[1,2-a]benzimidazoles." Synthesis 50, no. 11 (2018): 2131–49. http://dx.doi.org/10.1055/s-0036-1589533.

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Pyrido[1,2-a]benzimidazole is one of the most important azaheterocyclic compounds consisting of three fused aromatic rings. Molecules containing this core have displayed a wide range of applications in the field of medicinal chemistry. The synthesis of pyrido[1,2-a]benzimidazole and its derivatives has attracted organic chemists because of its tremendous utility in interdisciplinary branches of chemistry. In this context, this review discusses the main advances in the synthesis of pyrido[1,2-a]benzimidazoles via metal-mediated and metal-free reactions from 2000 to 2016.1 Introduction2 Syntheti

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46

Nguyen, Hoang-Phuc, Thi Kim Chi Huynh, Khac-Minh Thai, and Thi-Kim-Dung Hoang. "QSAR modeling and molecular docking studies on benzimidazole derivatives as anticancer agents." Vietnam Journal of Science and Technology 60, no. 6 (2022): 993–1004. http://dx.doi.org/10.15625/2525-2518/17072.

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Abstract. The triple-negative breast cancer cell line MDA-MB-231 has been known as one of the most tenacious cancer cancer cells and paid attention by many researchers. A two-dimension quantitative structure-activity relationship (2D-QSAR) model of 131 benzimidazole derivatives was developed to relate the chemical–biological interactions and predicted the half maximal inhibitory concentration (IC50) against MDA-MB-231 cell line. The 2D-QSAR model was obtained satisfactory internal and external validation parameters such as the square of correlation coefficient R2 = 0.904 and concordance correl

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Singh, Namrata, Annamalai Pandurangan, Kavita Rana, Preeti Anand, Arsad Ahamad, and Amit Kumar Tiwari. "Benzimidazole: A short review of their antimicrobial activities." International Current Pharmaceutical Journal 1, no. 5 (2012): 110–18. http://dx.doi.org/10.3329/icpj.v1i5.10284.

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Benzimidazole is the heterocyclic compound formed from benzene and imidazole ring containing nitrogen, oxygen sulphor and its derivatives are of wide interest because of their diverse biological activity and clinical applications, they are remarkably effective compounds both with respect to their inhibitory activity and their favourable selectivity ratio. Reported nucleus is a constituent of vitamin-B12. Benzimidazoles are regarded as a promising class of bioactive heterocyclic compounds that exhibit a range of biological activities like anti-microbial, anti-viral, anti-diabetic, anti-cancer a

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El Bialy, Serry Atta, Basem Mansour, Waleed Abdelhakeem Bayoumi, Amira Taman, and Hassan Mohammed Eissa. "Novel 2-(5-Aryl)thiophen-2-yl)benzimidazoles; Design, Synthesis and In vitro Evaluation Against Cercarial Phase of Schistosoma mansoni." Letters in Drug Design & Discovery 17, no. 11 (2020): 1432–38. http://dx.doi.org/10.2174/1570180817999200523181211.

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Background: Literature survey has pointed out that Benzimidazoles represent an interesting class of anthelmintics, of which several potent members were developed. Objective: Benzimidazoles hybridized with pharmacophoric moieties possessing anthelmintic activity were designed, synthesized to be evaluated against cercaria. Methods: Structural modification was achieved through 2- and 5-positions. Moreover, an in vitro cercarial assay was adopted to evaluate target compounds. Results and Discussion: Biological screening revealed that compound 3h showed significant activity with a survival index of

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Mohammed, Samar M., Wesam S. Shehab, Abdul-Hamid M. Emwas, et al. "Eco-Friendly Synthesis of 1H-benzo[d]imidazole Derivatives by ZnO NPs Characterization, DFT Studies, Antioxidant and Insilico Studies." Pharmaceuticals 16, no. 7 (2023): 969. http://dx.doi.org/10.3390/ph16070969.

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Benzimidazoles are classified as a category of heterocyclic compounds. Molecules having benzimidazole motifs show promising utility in organic and scientific studies. A series of mono-substituted benzimidazoles were synthesized by ZnO-NPs via cyclocondensation between substituted aromatic aldehydes and o-phenylene diamine. The synthesized compounds were characterized and compared with the traditional methods. The nano-catalyzed method displayed a higher yield, shorter time and recyclable catalyst. The DFT study and antioxidant activity were investigated for benzo[d]imidazole derivatives. Compo

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Prasada Rao, Chennu Maruthi Malya. "Molecular docking and dynamic simulations of benzimidazoles with beta-tubulins." Bioinformation 17, no. 3 (2021): 404–12. http://dx.doi.org/10.6026//97320630017404.

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It is of interest to document the molecular docking and dynamic simulations of benzimidazoles with beta-tubulins in the context of anthelmintic activity. We document the compound BI-02 (2-(3,4-dimethyl phenyl)-1H-1,3-benzimidazole (BI-02) with optimal bindig features compared to the standard molecule albendazole (7.0 Kcal/mol) with binding energy -8.50 Kcal/mol and PIC50 value 583.62 nM.

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