Antimicrobial potential of 1H-benzo[d]imidazole scaffold: a review

Tahlan, Sumit; Kumar, Sanjiv

doi:10.1186/s13065-019-0521-y

Cited by 44 publications

(21 citation statements)

References 53 publications

(55 reference statements)

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“…A similar study on a series of synthesized benzothiazole derivatives reported potent antimicrobial activity against some bacterial strains, namely Bacillus subtilis, Escherichia coli, Streptomyces griseus and also found effective against some fungal strains, namely Candida albicans and Aspergillus niger (Soni et al, 2010). Also, various previous studies showed that some benzimidazole and benzoxazole exhibited excellent results against some bacterial strains and benzothiazole against some fungal strains (Padalkar et al, 2016;Tahlan et al, 2019).…”

Section: Antimicrobial Evaluationmentioning

confidence: 74%

Evaluation of some new synthesis benzothiazole and benzimidazole Derivatives as potential antimicrobial and anticancer agents

Elaziz¹

2020

Int. j. adv. appl. sci.

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There is an urgent global need to develop new antimicrobial and anti-cancer drugs. In the current study, the biological evaluation of some synthesized phenylsulfonyl of benzothiazole and benzimidazole moiety-containing pyrazolo [5, 1-c]-l, 2, 4-triazine derivative [6, 7, 11.12, 16 and 17], arylhydrazone derivatives and pyridazine derivative [20, 21, 25, 26, 29 and 29] was carried out for antimicrobial and anticancer activity. The synthesized compounds containing pyrazolo [5, 1-c]-l, 2, 4-triazine derivative [6, 7] exhibited higher activity against Staphylococcus aureus compared with control drug Chloramphenicol. While arylhydrazones 20 and 21 were found to be equal to the control drug. For antifungal activity, the compounds 6, 7, 20 and 21 were possessed the same potency as cycloheximide against Aspergillus fumigatus. The anticancer activity on Hepatocellular carcinoma (HEPG2) of the compounds 6, 7, 20 and 21 exhibited excellent activities, more potent than the reference drug. The findings of this study are worthwhile; however, further pharmaceutical and toxicological studies are recommended to be carried out.

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Section: Antimicrobial Evaluationmentioning

confidence: 74%

Evaluation of some new synthesis benzothiazole and benzimidazole Derivatives as potential antimicrobial and anticancer agents

Elaziz¹

2020

Int. j. adv. appl. sci.

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“…Benzimidazole derivatives during literature survey found that, 2-substituted analogues are more dynamic and hence composition and synthesis of 2-substituted compounds are remarkable sector of research (Tahlan et al, 2019). Various 1-(substituted-methyl)-2(substituted-phenyl) benzimidazole derivatives were synthesized and reported for their antibacterial activity against bacterial strains of S. aureus, B. pumillus and P. aeruginosa, Compound (7a) revealed most potent antibacterial activity (Enumula et al, 2014).…”

Section: Anti-bacterial Activitymentioning

confidence: 99%

“…It contains benzene and imidazole ring fused together at 4 and 5 position (Palit et al, 2016). They show both acidic and basic properties due to amphoteric nature of nitrogen atoms (Tahlan et al, 2019). It is a privileged macromolecule and entitled pharmacophore in medicinal chemistry.…”

Section: Introductionmentioning

confidence: 99%

A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold

Babbar

Swikriti

Arora

2020

JPTRM

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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.

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“…Imidazole-based heterocycles are a common motif found in both natural and synthetic compounds, present in several clinically approved drugs [ 1 , 2 , 3 ]. In particular, the benzimidazole moiety is a relevant scaffold for multiple applications in clinic, showing antiulcer, antihypertensive, antiparasitic, anticancer, antifungal, and antibacterial activities [ 4 , 5 ]. For instance, ridinilazole, a recently developed antibacterial containing the benzimidazole scaffold, is currently in phase III clinical trials and has shown great promise for treating Clostridioides difficile infections [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Computationally Designed 2,5(6)-Benzimidazole Derivatives via Pd-Catalyzed Reactions for Potential E. coli DNA Gyrase B Inhibition

2021

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A pharmacophore model for inhibitors of Escherichia coli’s DNA Gyrase B was developed, using computer-aided drug design. Subsequently, docking studies showed that 2,5(6)-substituted benzimidazole derivatives are promising molecules, as they possess key hydrogen bond donor/acceptor groups for an efficient interaction with this bacterial target. Furthermore, 5(6)-bromo-2-(2-nitrophenyl)-1H-benzimidazole, selected as a core molecule, was prepared on a multi-gram scale through condensation of 4-bromo-1,2-diaminobenzene with 2-nitrobenzaldehyde using a sustainable approach. The challenging functionalization of the 5(6)-position was carried out via palladium-catalyzed Suzuki–Miyaura and Buchwald-Hartwig amination cross-coupling reactions between N-protected-5-bromo-2-nitrophenyl-benzimidazole and aryl boronic acids or sulfonylanilines, with yields up to 81%. The final designed molecules (2-(aminophen-2-yl)-5(6)-substituted-1H-benzimidazoles), which encompass the appropriate functional groups in the 5(6)-position according to the pharmacophore model, were obtained in yields up to 91% after acid-mediated N-boc deprotection followed by Pd-catalyzed hydrogenation. These groups are predicted to favor interactions with DNA gyrase B residues Asn46, Asp73, and Asp173, aiming to promote an inhibitory effect.

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Antimicrobial potential of 1H-benzo[d]imidazole scaffold: a review

Cited by 44 publications

References 53 publications

Evaluation of some new synthesis benzothiazole and benzimidazole Derivatives as potential antimicrobial and anticancer agents

Evaluation of some new synthesis benzothiazole and benzimidazole Derivatives as potential antimicrobial and anticancer agents

A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold

Synthesis of Computationally Designed 2,5(6)-Benzimidazole Derivatives via Pd-Catalyzed Reactions for Potential E. coli DNA Gyrase B Inhibition

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