Synthesis, <i>In Silico</i> Designing, Microbiological Evaluation and Structure Activity Relationship of Novel Amide Derivatives of 1-(2,4-Dinitrophenyl)-2-(3-Methylbenzo[b]Thiophen-6-yl)-1H-Benzo[d]Imidazole-5-Carboxylic Acid

Hooda, Tanuj; Sharma, Sunil; Goyal, Nupur

doi:10.1080/10406638.2020.1869793

Cited by 6 publications

References 18 publications

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Synthesis, Properties, and Biological Applications of Benzothiophene

Wable,

Mascarenhas,

Akolkar

et al. 2024

S-Heterocycles

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Benzothiophene is a heterocyclic aromatic compound containing sulfur as a heteroatom in the five-membered ring, which is fused with benzene. Medicinal chemistry has shown a great deal of interest in benzothiophene, as it showed various pharmacological properties and structural versatility. The synthesis of benzothiophene derivatives involves multiple strategies, with researchers using a variety of synthetic methodologies. Benzothiophene compounds exhibit a broad range of biological activities, making them attractive candidates for drug development. In terms of their biological and physiological properties, viz. antimicrobial, anti-inflammatory, anti-anxiety, anti-arrhythmic, anti-psychotic, kinase-inhibiting, and anticancer properties, they are remarkably effective compounds. The benzothiophene scaffold has been found in medicinal drugs, such as zileuton, benzothiophenylcyclohexylpiperidine (BTCP), raloxifene, and sertaconazole. In addition, it is used to produce hues, such as thioindigo. Considering the above-mentioned facts, this chapter explores the synthesis and the potential applications of benzothiophenes in drug development and their impact on various aspects of medicinal chemistry, such as analgesic, anti-inflammatory, anticancer, antioxidant, anti-tubercular, anti-HIV, anti-Parkinson, anti-convulsing, and anti-diabetic activities.

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Synthesis, Properties, and Biological Applications of Benzothiophene

Wable,

Mascarenhas,

Akolkar

et al. 2024

S-Heterocycles

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Thiophenes

2024

S-Heterocycles

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Neuroprotective Role of Ranolazine: ESR1 and NMDA Receptor Agonist in Traumatic Brain Injury in Drosophila melanogaster, In Silico and In Vivo Correlation

Parvesh,

Kumar,

Singh

et al. 2024

Indian Journal of Neurotrauma

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Objective In this study, a high-impact trauma (HIT) device was used for inducing moderate traumatic brain injury (TBI) in Drosophila melanogaster. Mechanical injuries in flies caused by rapid acceleration and assertion produce symptoms characteristics of TBI in humans. Materials and Methods Docking studies were carried out to check the binding affinity of the drug toward the receptors. Various oxidative stress parameters, catalase level, glutathione level, superoxide dismutase (SOD) level, malondialdehyde (MDA), and nitric oxide levels, were measured. The mortality index and neuroprotective potential were carried out in TBI in D. melanogaster models. Results In the current study, there was an increase in oxidative stress following TBI as evidenced by a significant decrease in the catalase, glutathione, and SOD levels and increase in the level of MDA and nitric oxide after 24 hours. Antioxidant enzymes, catalase and glutathione peroxidase, have a dominant role in TBI. Docking studies were carried out on estrogen receptor 1 (pdb: 1TVO and 1UOM) and NDMA receptor (pdb: 3QEL) as agonist showing the binding affinity of the drug toward the receptors. In comparison to the vehicle-treated group, there was a dose-dependent significant increase in the SOD level and percentage climbing along with a decrease in the MDA level and total protein content. The mortality index was also observed at three concentrations of ranolazine (1, 2, and 4 mg/mL) in D. melanogaster homogenate. These findings suggest that ranolazine has a good neuroprotective potential in the treatment of TBI in the D. melanogaster model. Conclusion Present study concluded the scientific evaluation of neuroprotective potential of ranolazine in the treatment of TBI in the D. melanogaster model.

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Synthesis, In Silico Designing, Microbiological Evaluation and Structure Activity Relationship of Novel Amide Derivatives of 1-(2,4-Dinitrophenyl)-2-(3-Methylbenzo[b]Thiophen-6-yl)-1H-Benzo[d]Imidazole-5-Carboxylic Acid

Cited by 6 publications

References 18 publications

Synthesis, Properties, and Biological Applications of Benzothiophene

Synthesis, Properties, and Biological Applications of Benzothiophene

Thiophenes

Neuroprotective Role of Ranolazine: ESR1 and NMDA Receptor Agonist in Traumatic Brain Injury in Drosophila melanogaster, In Silico and In Vivo Correlation

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