A Review On Substituted Benzimidazoles: Biologically Active Compounds

Madawali, Indira. M.; N, Gaviraj E.; Kalyane, Navanath V.; Shivakumar, B.

doi:10.46624/ajptr.2019.v9.i3.021

Cited by 9 publications

(4 citation statements)

References 18 publications

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“…Karale et al synthesized bis-benzimidazole-1,2,4-triazole hybrids 102a-102e (Scheme 25) in four steps from 7-methyl-2-propyl-3H-benzo[d]imidazole-5-carboxylic acid. All compounds 102 did not show antimicrobial activity against the strains tested, C. albicans, A. fumigatus, S. aureus, and E. coli [156,157]. 10 reveal that compounds 109a, 109c and 109e exhibited satisfactory effects against S.aureus and E.coli, while compounds 109b 109f, and 109g showed moderate activity against the same microbes.…”

Section: Kankate Et Al Reported the Synthesis Of Hybrids 73a-73l (Sch...mentioning

confidence: 92%

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

Marinescu

2023

Antibiotics

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Bacterial infections have attracted the attention of researchers in recent decades, especially due to the special problems they have faced, such as their increasing diversity and resistance to antibiotic treatment. The emergence and development of the SARS-CoV-2 infection stimulated even more research to find new structures with antimicrobial and antiviral properties. Among the heterocyclic compounds with remarkable therapeutic properties, benzimidazoles, and triazoles stand out, possessing antimicrobial, antiviral, antitumor, anti-Alzheimer, anti-inflammatory, analgesic, antidiabetic, or anti-ulcer activities. In addition, the literature of the last decade reports benzimidazole-triazole hybrids with improved biological properties compared to the properties of simple mono-heterocyclic compounds. This review aims to provide an update on the synthesis methods of these hybrids, along with their antimicrobial and antiviral activities, as well as the structure–activity relationship reported in the literature. It was found that the presence of certain groups grafted onto the benzimidazole and/or triazole nuclei (-F, -Cl, -Br, -CF3, -NO2, -CN, -CHO, -OH, OCH3, COOCH3), as well as the presence of some heterocycles (pyridine, pyrimidine, thiazole, indole, isoxazole, thiadiazole, coumarin) increases the antimicrobial activity of benzimidazole-triazole hybrids. Also, the presence of the oxygen or sulfur atom in the bridge connecting the benzimidazole and triazole rings generally increases the antimicrobial activity of the hybrids. The literature mentions only benzimidazole-1,2,3-triazole hybrids with antiviral properties. Both for antimicrobial and antiviral hybrids, the presence of an additional triazole ring increases their biological activity, which is in agreement with the three-dimensional binding mode of compounds. This review summarizes the advances of benzimidazole triazole derivatives as potential antimicrobial and antiviral agents covering articles published from 2000 to 2023.

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Section: Kankate Et Al Reported the Synthesis Of Hybrids 73a-73l (Sch...mentioning

confidence: 92%

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

Marinescu

2023

Antibiotics

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“…This problem was solved by the improved Phillips method for synthesizing the benzimidazole by using dilute mineral acid at lower temperature with o-phenylenediamine and organic acid as starting materials (scheme 1). The yield of this method can be increase by the use of aromatic acid also 11,12 . antibacterial and antifungal compounds.…”

Section: Phillips Methods Of Synthesismentioning

confidence: 99%

A systematic review on diverse synthetic route and pharmacological activities of benzimidazole as optimized lead

Thapa¹,

NARGUND²,

Biradar³

2022

juc

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The aim of this review is to provide the systematic information of synthetic scheme and biological activity of synthesized benzimidazole derivatives. Benzimidazole is widely used lead molecule for the synthesis of various types of pharmacologically active moiety. It is heterocyclic aromatic fused colorless solid having molecular mass of 118.053 g/mol. It is basic in nature and can be served as ligand in coordination chemistry. It is bioactive compound showed various pharmacological activity till now viz. anthelmintics (albendazole, mebendazole), proton pump inhibitors (omeprazole, pantoprazole), antibiotics, antiprotozoal, antifungal, anticancer, anti-viral, anti-oxidant, anti-inflammatory etc. Various synthetic route by various methods is also already reported. Some of them are traditional convenient method, microwave reactor method, solvent free synthesis method, green synthesis method. Due to its wide variety of biological action and the similarity with biomolecule, it is frequently taken as lead for new drug discovery

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“…According to recent research, benzimidazole derivatives act as a versatile core structure for the synthesis of novel compounds with powerful biological actions. It is the most popular term for the series parent molecule, this ring is also known as 1,3‐benzimidazole [18] . Benzimidazole derivatives of the heterocyclic class are also being highlighted by medicinal chemists due to their extensive range of pharmacological potentials [19] .…”

Section: Introductionmentioning

confidence: 99%

“…It is the most popular term for the series parent molecule, this ring is also known as 1,3-benzimidazole. [18] Benzimidazole derivatives of the heterocyclic class are also being highlighted by medicinal chemists due to their extensive range of pharmacological potentials. [19] On the other hand, Quinoline is a benzo-fused heterocyclic molecule widely described as a fundamental component of naturally occurring compounds and primarily responsible for therapeutic activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, In Silico and In Vivo Evaluation of Benzimidazole‐Bearing Quinoline Schiff Bases as New Anticonvulsant Agents

et al. 2023

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Nitrogen‐containing hybrid heterocyclic compounds have been gaining attention in the field of drug discovery and development due to their diverse pharmacological activities and relatively low toxicity. This study aimed to synthesize a series of new quinoline‐bearing amino acid‐derived benzimidazole derivatives i. e. 3‐{[1‐(1H‐Benzoimidazol‐2‐yl)‐subsituted‐methyl}‐4a,8a‐ dihydro‐1H‐quinoline‐2‐one, and 3‐{[1‐(1H‐Benzoimidazol‐2‐yl)‐substituted‐methyl}‐3H‐ quinoline‐2‐thione. These compounds were synthesized by the condensation of 2‐oxo‐1,2‐dihydro‐quinoline‐3‐ carbaldehyde and 2‐the oxo‐1,2‐dihydro‐quinoline‐3‐carbaldehyde with various substituted 1‐(1H‐benzimidazole‐2‐yl)‐methylamine. After synthesizing the compound, it was subjected to various characterization techniques such as IR, 1HNMR, 13CNMR, and Mass spectroscopy. The synthesized compounds were evaluated for their potential as an anticonvulsant using the subcutaneous Pentylenetetrazol (scPTZ) method, and the results were compared with those obtained for phenytoin and carbamazepine, which were used as standard drugs. Among all the screened derivatives 4 d, 4 e, 5 a, and 5 b were found to be the most potent as compared to conventional drugs (phenytoin and carbamazepine). Also, the molecular docking analysis of the synthesized compounds showed that they share the same mechanism of action as phenytoin and carbamazepine, which involves the inhibition of voltage‐gated sodium channels. Additionally, the analysis revealed that these compounds also inhibit the NMDA receptor. Overall, the development of nitrogen‐containing hybrid heterocyclic compounds has the potential to significantly contribute to the discovery and development of new drugs with improved efficacy, selectivity, and safety profiles.

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A Review On Substituted Benzimidazoles: Biologically Active Compounds

Cited by 9 publications

References 18 publications

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

A systematic review on diverse synthetic route and pharmacological activities of benzimidazole as optimized lead

Synthesis, Characterization, In Silico and In Vivo Evaluation of Benzimidazole‐Bearing Quinoline Schiff Bases as New Anticonvulsant Agents

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