Microwave Assisted Liquid Phase Synthesis of Benzimidazolo Benzothiophenes for Antimicrobial Activity

Kini, Deepthi. D.; Kumar, Harish; Ghate, Manjunath

doi:10.1155/2009/934706

Cited by 8 publications

(3 citation statements)

References 10 publications

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“…Synthesis of 2-(3-methylbenzo [b]thiophen-6-yl)-1-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxylic acid outlined in Scheme 1 (Figure 1). 21,22 Structural part of compounds was in confirmed by Mass spectra, 23 1 H NMR and 13 CNMR 24 and elemental analysis which were found in full agreement with their structures. Detection of reaction completion was done by single spot TLC under UV lamp.…”

Section: Methodsmentioning

confidence: 57%

Synthesis, in-silico Designing, SAR and Microbiological Evaluation of Novel Amide Derivatives of 1-(4-Nitrophenyl)-2-(3-methylbenzo[b] thiophen-6-yl)-1H-benzo[d]imidazole-5-carboxylic Acid

Hooda¹,

Sharma²,

Goyal³

2020

IJPER

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Background: Due to this increasing predicament of antibiotic confrontation, the lot of distinct antibiotics available is dwindling and there are only smatterings of new antibiotics in the drug development channel. Therefore, an intense necessitate for new antimicrobial drugs. In current study, we have synthesized the new derivatives with the help of molecular docking studies and investigated antimicrobial activities. Methods: By focusing the enzymes i.e. aminoacyl-tRNA synthetase (AaRS) and tyrosyl-tRNA synthetase, new amides of 2-(3-methylbenzo[b]thiophen-6-yl)-1-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxylic acid were synthesized and inhibition by docking study precedence to antimicrobial action. Studies were accomplished on a designed library of amide derivatives with the help of docking softwares i.e. AutoDock Vina 4.2 and Schrodinger's maestro package against crystal structure of enzymes (PDB ID: 1wny.PDBQT and1jil.PDBQT). Based upon their dock score, superlative 23 focused amide derivatives of 2-(3-methylbenzo[b]thiophen-6-yl)-1-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxylic acid were synthesized and further Conclusion: In-vitro results revealed that a large number of synthesized compounds having good antimicrobial activity and dock score can be used for in vivo studies for future. In-silico studies and in vitro results comply with each other.

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Section: Methodsmentioning

confidence: 57%

Synthesis, in-silico Designing, SAR and Microbiological Evaluation of Novel Amide Derivatives of 1-(4-Nitrophenyl)-2-(3-methylbenzo[b] thiophen-6-yl)-1H-benzo[d]imidazole-5-carboxylic Acid

Hooda¹,

Sharma²,

Goyal³

2020

IJPER

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“…[26] In view of the importance of benzimidazoles and benzothiophene, Kini et al [27] designed ands ynthesized novel derivatives. [26] In view of the importance of benzimidazoles and benzothiophene, Kini et al [27] designed ands ynthesized novel derivatives.…”

Section: 25-trisubstituted Benzimidazolesmentioning

confidence: 99%

Recent Development of Benzimidazole‐Containing Antibacterial Agents

Song

2016

ChemMedChem

128

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Clinically significant antibiotic resistance is one of the greatest challenges of the twenty-first century. However, new antibacterial agents are currently being developed at a much slower pace than our growing need for such drugs. Given their diverse biological activities and clinical applications, many bioactive heterocyclic compounds containing a benzimidazole nucleus have been the focus of interest for many researchers. The benzimidazole nucleus is a structural isostere of naturally occurring nucleotides. This advantage allows benzimidazoles to readily interact with the various biopolymers found in living systems. In view of this situation, much attention has been given to the exploration of benzimidazole-based antibacterial agents, leading to the discovery of many new chemical entities with intriguing profiles. In this minireview we summarize novel benzimidazole derivatives active against various bacterial strains. In particular, we outline the relationship between the structures of variously modified benzimidazoles and their antibacterial activity.

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“…N‐Aryl substituted benzimidazoles manifest various kinds of biological activity: antiviral, antituberculous, antibacterial, antileishmaniasis . They can be antagonists and agonists of hormonal, intranuclear and other receptors.…”

Section: Introductionmentioning

confidence: 99%

Recyclization‐Isomerization in the Reduction of 1‐(2‐Nitro(het)aryl)benzimidazoles

2020

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The regularities of reductive recyclization‐isomerization of 1‐(2‐nitro(het)aryl)‐substituted benzimidazoles discovered by the authors have been studied. The structure of the intermediate has been identified and the isomerization process has been found to be reversible. The shift of equilibrium between the resulting isomers is affected by the reaction temperature and time, the amount of hydrogen chloride in the reaction mixture and the substrate structure. According to the suggested reaction mechanism, the amino group formed upon reduction reacts with the electron‐deficient α‐carbon atom in an imidazole by an AdN reaction. Based on these studies, a method for the functionalization of benzimidazoles has been developed. This young methodology has been used to synthesize hitherto unknown benzimidazole derivatives that are difficult to obtain by other methods.

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Microwave Assisted Liquid Phase Synthesis of Benzimidazolo Benzothiophenes for Antimicrobial Activity

Cited by 8 publications

References 10 publications

Synthesis, in-silico Designing, SAR and Microbiological Evaluation of Novel Amide Derivatives of 1-(4-Nitrophenyl)-2-(3-methylbenzo[b] thiophen-6-yl)-1H-benzo[d]imidazole-5-carboxylic Acid

Synthesis, in-silico Designing, SAR and Microbiological Evaluation of Novel Amide Derivatives of 1-(4-Nitrophenyl)-2-(3-methylbenzo[b] thiophen-6-yl)-1H-benzo[d]imidazole-5-carboxylic Acid

Recent Development of Benzimidazole‐Containing Antibacterial Agents

Recyclization‐Isomerization in the Reduction of 1‐(2‐Nitro(het)aryl)benzimidazoles

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