Synthesis, Characterization, and Biological Evaluation of Benzimidazole Derivatives as Potential Anxiolytics

Nannapaneni, D; Av, Gupta; Reddy, M. Ram; RCh, Sarva

doi:10.4103/0975-1483.66809

Cited by 28 publications

(4 citation statements)

References 25 publications

(21 reference statements)

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“…The clinical application of benzimidazole-containing drugs includes the fungicide and antiparasitic thiabendazole, the antihistamine clemizole, the anti-ulcerative omeprazole, the anti-hypertensive telmisartan, the antiviral Hoechst 33342, and the anticancer bendastumide [ 89 ]. Over the years, several methods were studied for the preparation of benzimidazole derivatives, involving the reaction between o-phenylenediamines and carboxylic acids or derivatives [ 90 ].…”

Section: Deep Eutectic Systemsmentioning

confidence: 99%

How Can Deep Eutectic Systems Promote Greener Processes in Medicinal Chemistry and Drug Discovery?

Domingues,

Duarte,

Jesus

2024

Pharmaceuticals

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Chemists in the medicinal chemistry field are constantly searching for alternatives towards more sustainable and eco-friendly processes for the design and synthesis of drug candidates. The pharmaceutical industry is one of the most polluting industries, having a high E-factor, which is driving the adoption of more sustainable processes not only for new drug candidates, but also in the production of well-established active pharmaceutical ingredients. Deep eutectic systems (DESs) have emerged as a greener alternative to ionic liquids, and their potential to substitute traditional organic solvents in drug discovery has raised interest among scientists. With the use of DESs as alternative solvents, the processes become more attractive in terms of eco-friendliness and recyclability. Furthermore, they might be more effective through making the process simpler, faster, and with maximum efficiency. This review will be focused on the role and application of deep eutectic systems in drug discovery, using biocatalytic processes and traditional organic chemical reactions, as new environmentally benign alternative solvents. Furthermore, herein we also show that DESs, if used in the pharmaceutical industry, may have a significant effect on lowering production costs and decreasing the impact of this industry on the quality of the environment.

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Section: Deep Eutectic Systemsmentioning

confidence: 99%

How Can Deep Eutectic Systems Promote Greener Processes in Medicinal Chemistry and Drug Discovery?

Domingues,

Duarte,

Jesus

2024

Pharmaceuticals

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“…and the minor amine υ (N-H), respectively. 16 A band has appeared in the spectrum of the LH, which is an important one whose appearance indicates the formation of the LH is the azomethine group υ(C=N) belonging to the Schiff base, 17 that appeared at 1674 cm -1 , while the band of the carbonyl group presents in the reactants before the reaction disappears. The bands at (1697 and 1658 cm -1 ) belong to the carbonyl group υ (C=O) carboxylic acid and the azomethine group υ (C=N) benzothiazole ring.…”

Section: Infra-red Spectramentioning

confidence: 99%

Evaluation of the Eff ectiveness of the Copper (II) Complex with a New Ligand derived from Benzothiazole and Anthranilic Acid as Anticancer and Antioxidant

Ali¹,

Jamel²

2023

IJDDT

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Four steps were used to convert 2-mercaptobenzothiazole into the new ligand (2-((2-((4-(1-((4’-(benzothiazol-2-ylamino)- [1,1’-biphenyl]-4-yl)imino) ethyl) phenyl)imino)-1,2diphenylethylidene) amino)benzoic acid (LH) type of schiff bases: The fi rst step included preparing compound (A) N-(benzothiazol-2-yl)-[1, 1’-biphenyl]-4, 4’-diamine by the reaction 2-mercaptobenzothiazole with benzidine. The second step was prepared the compound(B) 2 OXO-1, 2-diphenylethylidene) amino) benzoic -(( 2- acid by the reacting anthranilic acid with benzil As for the third step, it included the reaction of the product of the fi rest step with 4-aminoacitophenon and the formation compound (C). The fourth step was the preparation ligand (LH) by reacting compound(B) with compound (C). Fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), UV-vis, melting points, molar conductivity, CHN, atomic absorption, magnetic sensitivity, and other measurements were used to determine the structure of the ligand (LH) and its complex with copper (II). The MTT method was used to evaluate the activity of the ligand (LH) and its complex with copper (II) in-vitro as an anticancer (human breast cancer (MCF7). Nd (MTT) assay was used to evaluate the ligand schiff base in-vitro anticancer activity of a Cu(II) complex against human breast cancer MCF7

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“…The generated ligand values can be visualized. The compounds showed better scores [26,27] (Table 5).…”

Section: Procedures For Aerobic Mic Testmentioning

confidence: 99%

Synthesis, in silico studies and antibacterial activity of some novel 2-substituted benzimidazole derivatives

Chintakunta¹,

Meka²

2020

Futur J Pharm Sci

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Background The o-phenylenediamine is a versatile starting material for several compounds. Synthesized o-phenylenediamine and amino acids (glycine, alanine, aspartic acid, and l-proline) undergo condensation via Phillips reaction. The synthesized compound showed the promising antibacterial activity of Bacillus subtilis and Pseudomonas aeruginosa at the concentration of 100, 50, 25, 12.5, 6.25, 3.12, 1.6, 0.8, 0.4, and 0.2 μg/ml. Ciprofloxacin was used as standard drug. Synthesis of benzimidazole derivatives was carried out and purified by recrystallization process using ethanol. Substituted derivatives were characterized by melting point, TLC and spectroscopic methods include FT-IR and 1H-NMR. Results In silico studies were adopted for synthetic derivatives by Molinspiration, ChemDraw, and online software tool. Minimum inhibitory concentration (MIC) values of B. subtilis and P. aeruginosa were reported, and benzimidazole ligands and Molinspiration scores were generated and listed. Conclusion The more negative values indicate a higher binding affinity. The generated ligand observations can be visualized. Physical constants of synthesized derivates such as solubility and melting point were determined. Bioactivity scores were noted for different derivatives and predicted percentage absorption in the gut. The antibacterial activity was performed using the MIC method (aerobic).

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Synthesis, Characterization, and Biological Evaluation of Benzimidazole Derivatives as Potential Anxiolytics

Cited by 28 publications

References 25 publications

How Can Deep Eutectic Systems Promote Greener Processes in Medicinal Chemistry and Drug Discovery?

How Can Deep Eutectic Systems Promote Greener Processes in Medicinal Chemistry and Drug Discovery?

Evaluation of the Eff ectiveness of the Copper (II) Complex with a New Ligand derived from Benzothiazole and Anthranilic Acid as Anticancer and Antioxidant

Synthesis, in silico studies and antibacterial activity of some novel 2-substituted benzimidazole derivatives

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