In the last 2-3 decades, the broad research in the application of benzimidazole derivatives
made it important for mankind. Many scientists have worked on benzimidazole derivatives and they
found that this compound has a diverse role in the field of medicinal chemistry. Few benzimidazole derivatives
are currently in the market as a drug candidate against various diseases. Moreover, the benzimidazole
derivatives exhibit pharmacological activities such as anti-tuberculosis, anti-malarial, antihistamine,
antimicrobial, antiviral, antidiabetic, anticancer, anti-fungal, anti-inflammatory, analgesic,
anti-HIV, etc. In this review, we have summarized various derivatives of benzimidazole which have
been prepared by many researchers to understand the chemistry as well as diverse pharmacological activities.
These findings may lead the scientists who are working in the field of medicinal chemistry to
the development of benzimidazole based drug candidates in the future.
Nitration of aromatic compounds represents a powerful and widely used transformation that allows introducing nitro group into aromatic systems. New synthetic strategies for aromatic nitration are deeply needed, including highly efficient and selective nitration methods. Aromatic nitration plays an important part in the industry, as the main use of nitration is to produce important products such as dyes & intermediate compounds, drugs, and Agrochemicals. The electrophilic aromatic nitration is most studied and important transformation in industrial process. This review will describe different possible methodologies that apply to this fundamental transformation with special attention to the most recent development that lasted from 2017–2020. The main pros and cons of recent nitration methods are briefly described with their specific reaction mechanism and highlighting the most important feature of the present aromatic nitration method.
A novel series of fluorine‐containing quinoline hybrid thiosemicarbazide analogues (8a–8l) were synthesized and tested for their biological activities. The antibacterial results demonstrated that compounds 8d and 8l [minimal inhibitory concentration (MIC) 62.5 μg/mL] were shown to have higher biological activity than ampicillin against Escherichia coli. Compound 8b (MIC 25 μg/mL) was shown to have the highest activity than was ampicillin against Staphylococcus aureus. The antifungal results demonstrated that compound 8j (MIC 100 μg/mL) has shown good activity. Most of the targeted compounds have shown potent antimalarial activity. Compounds 8d (0.19 μg/mL), 8g (0.30 μg/mL), 8h (0.36 μg/mL), 8k (0.10 μg/mL), 8l (0.28 μg/mL), 8k (0.10 μg/mL), and 8l (0.28 μg/mL) have notable activity than does the reference drug quinine. Compounds 8d (0.27 μg/mL), 8g (0.30 μg/mL), and 8k (0.17 μg/mL) have shown excellent activity against chloroquine‐resistant strain. The MTT assay performed on peripheral blood lymphocyte cultures showed a high percentage of lymphocyte viability [8d (99.64), 8g (99.46), 8h (98.83), and 8k (99.51)] at a maximum dose (10 μg/mL), depicting no cytotoxicity of these compounds on human lymphocytes in vitro. A molecular docking study was performed on Pf‐DHFR‐TS inhibitor. A molecular dynamics study has shown compound 8g to have better affinity with protein. ADME‐Tox and pharmacophore study of synthesized compounds suggested prediction of active site.
In the present study, a novel series of N‐((substituted)carbamothioyl)‐2,4‐dimethylquinoline‐3‐carboxamide (7a‐7s) was synthesized by microwave‐assisted method. Structure of these derivatives was examined by spectroscopic techniques such as 1H NMR, 13C NMR, FT‐IR, and ESI‐MS. Further, the novel synthesized compounds were evaluated for their in‐vitro biological activities against antibacterial, antifungal, antimalarial, and antituberculosis activity as well as for in‐silico study. The antimalarial results demonstrated that compounds 7c and 7q (0.02 μg/mL) have notable potency against Plasmodium falciparum compared with chloroquine (0.02 μg/mL); compounds 7l (0.10 μg/mL), 7e, 7s (0.19 μg/mL), 7b, 7p (0.15 μg/mL), 7a, 7f, and 7f (0.25 μg/mL) also exhibited good activity against P. falciparum compared with quinine (0.26 μg/mL) as standard drug. Docking was performed on PFDHFR‐TS, given the effect of compounds against the P. falciparum strain was excellent in comparison with standard drug. Molecular docking suggested that compounds 7b, 7i and 7c, 7e, and 7l closely bind with the active site of protein 3JSU and 4DP3, respectively, and compared with biological activity. We have also carried out molecular dynamics simulation on the best dock compound 7e complex with PDB: 3JSU to check the stability of docked complex and their molecular interaction. The calculated ADME‐Tox descriptors for the synthesized compounds validated good pharmacokinetics properties, suggesting that these compounds could be used as hit for the development of the new active agents.
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