ChemInform Abstract: Synthesis of 2‐[(4‐Amino or 2,4‐Diaminophenyl)sulfonyl] Derivatives of Benzimidazole, Benzothiazole and 6‐Methyluracil as Potential Antimicrobial Agents.

Ghoneim, K. M.; Essawi, M. Y. H.; Mohamed, Manal G.; Kamal, Amr; El‐Megid, R. M. Abd

doi:10.1002/chin.199909105

Cited by 3 publications

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“…Ghoneim et al in 1998, 41 prepared a series of 2-[(4-aminophenyl)sulphonyl] analogues and screened for the antimicrobial activity by using the agar diffusion method. It was found that all prepared compounds have significant antimicrobial activity, of which the compounds (64) and (65) were found to be the most active among all.…”

Section: Antimicrobial Activitymentioning

confidence: 99%

Significance of Benzimidazole analogues for the creation of novel molecules in drug discovery

Sharma¹,

Gupta²,

Gupta³

et al. 2023

10.5267/j.ccl

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Fused heterocyclic derivatives have become an important scaffold nowadays, which could be used as a template in drug development and medicinal chemistry. Benzimidazole moiety is an imperious aromatic heterocycle which is frequently present in naturally occurring products such as purines, vitamin B 12 and histidine as well as synthesized bioactive compounds, indomethacin and albendazole, for example. This study comprises widespread and comprehensive literature analysis on chemical reactivity and biological properties associated with Benzimidazole containing molecules. Benzimidazole ring structure possesses an extensive variety of pharmacological activities in several medications of therapeutic interest against a variety of diseases such as hypertension, malaria, cancer, microbial diseases, inflammatory disorders, etc. Furthermore, this fused heterocycle benzimidazole core might interact with various anions and cations in addition to biomolecules over different reactions in the human body, therefore exhibiting wide-ranging biological activities such as antineoplastic, antibacterial and antifungal, anti-inflammatory and analgesic, antihypertensive, antiviral and antidepressant. In this review, we are focusing on the chemistry and recent biological activities, designing approaches, and SAR (structure-activity relationship) data of different benzimidazole-based analogues during the past years.

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Section: Antimicrobial Activitymentioning

confidence: 99%

Significance of Benzimidazole analogues for the creation of novel molecules in drug discovery

Sharma¹,

Gupta²,

Gupta³

et al. 2023

10.5267/j.ccl

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A Review on Green Synthesis and Biological Activities of Medicinally Important Nitrogen and Oxygen Containing Heterocycles

Gulati

Singh

Sangwan

2023

COC

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Recently, the application of green chemistry for the formation of potential bioactive heterocyclic moieties has turned out to be the key area of research for organic chemists due to the growing concern over environmental issues. Therefore, the development of nonhazardous synthetic protocols gained the particular attention of synthetic chemists as a frontier task in the present scenario. Nowadays, microbial infections have been haunting human civilization since prehistoric times, resulting in many deaths worldwide. Cancer is a fatal and dreadful disease without any appropriate cure, thus threatening humanity in both the developing and developed worlds. Therefore, there is a critical requirement for the design and synthesis of new classes of compounds to circumvent these diseases. Heterocycles are unique precursors for the synthesis of various pharmaceuticals and agrochemicals, particularly those possessing N- or O- moieties. The methods to prepare heterocycles are of great importance in synthesizing organic compounds, especially the heterocycles found in natural products. The synthesis of nitrogen and oxygen-containing heterocycles viz. Coumarins, dihydropyrimidinones, imidazoles, isoxazoles, and benzimidazoles represent attractive and demanding work for chemists as these molecules have found extensive applications in several fields, such as materials science, analytical chemistry and most importantly in, medicinal chemistry. In this review paper, we focus on the synthetic strategy to prepare these types of heterocyclic compounds by green methods and discuss their various biological applications.

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Synthesis and Antimycobacterial Activity of Benzimidazole Derivatives

Mathapati¹,

Durgad²,

Singh³

et al. 2012

IND. DRU.

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In the present study, the objective is to synthesize novel compounds from the benzimidazole moiety,recognized for its various biological potentials. Chalcone being a very good synthon was utilized to combine with the benzimidazole moiety to design agents with significant antimycobacterial activity. Benzimidazole is formed when o-phenylene diamine is heated with organic acid i.e. formic acid; in presence of strong alkali sodium hydroxide it will gives benzimidazole. Benzimidazole was acetylated with acetyl chloride, the intermediate substituted chalcones were synthesized from acetylated benzimidazole, in order to synthesize different substituted aromatic aldehydes of the basic moiety, 1-sub. benzimidazole to obtain the different benzimidazole derivatives. Their structures were characterized by various spectral techniques like IR, NMR and MS. For the preliminary screening (antibacterial and antifungal)for antimicrobial activity, the test was performed by disc diffusion assay and determination of minimum inhibitory concentration (MIC) by broth dilution method. The antimycobacterial screening was performed against Mycobacterium tuberculosis by Almar blue assay (ABA) and Luciferase reporter phase (LRPA) techniques using isoniazid as the standard.

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ChemInform Abstract: Synthesis of 2‐[(4‐Amino or 2,4‐Diaminophenyl)sulfonyl] Derivatives of Benzimidazole, Benzothiazole and 6‐Methyluracil as Potential Antimicrobial Agents.

Cited by 3 publications

References 0 publications

Significance of Benzimidazole analogues for the creation of novel molecules in drug discovery

Significance of Benzimidazole analogues for the creation of novel molecules in drug discovery

A Review on Green Synthesis and Biological Activities of Medicinally Important Nitrogen and Oxygen Containing Heterocycles

Synthesis and Antimycobacterial Activity of Benzimidazole Derivatives

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