Synthesis, Anti-inflammatory, Analgesic and Antipyretic Activity of Novel 1,3,5-Trisubstituted Pyrazole Derivatives

doi:10.14233/AJCHEM.2019.21781

Paper

Synthesis, Anti-inflammatory, Analgesic and Antipyretic Activity of Novel 1,3,5-Trisubstituted Pyrazole Derivatives

Published May 25, 2019 · T. Padmini, B. R. Kamal

Asian Journal of Chemistry

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6

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0

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Abstract

A novel series of 1,3,5-trisubstituted pyrazole derivatives were synthesized by the cycloaddition reaction between the electron rich N-substituted aryl hydrazones and nitro-olefins. Different N-substituted aryl hydrazones (1a-j) on reacting with 4-methyl-β-nitrostyrene (2) in ethylene glycol or trifluoroethanol-trifluoro acetic acid mixture (for acid stable hydrazones) at 120 ºC, yielded various 1,3,5-trisubstituted pyrazoles (3a-j). The final products were characterized by spectral analysis using Mass, NMR and IR spectroscopy. All the products were assessed for their anti-inflammatory, analgesic and antipyretic activities on Swiss albino rats. All the compounds (3a-j) exhibited noteworthy defence against inflammation, nociception and hyperthermia. Compounds (3e and 3h) disclosed better antiinflammatory, analgesic and antipyretic activities while compound 3c had highest anti-inflammatory activity compared to the standard nimesulide.

Non-RCT

Animal Study

Study Snapshot

Novel 1,3,5-trisubstituted pyrazole derivatives show promising anti-inflammatory, analgesic, and antipyretic activities, with compounds 3e and 3h showing better results than standard nimesulide.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis, Anti-inflammatory, Analgesic and Antipyretic Activity of Novel 1,3,5-Trisubstituted Pyrazole Derivatives

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References

Design, synthesis and anticancer evaluation of novel pyrazole, pyrazolo[3,4-d]pyrimidine and their glycoside derivatives

Novel pyrazole, pyrazolo[3,4-d]pyrimidine and their glycoside derivatives show promising antitumor activity against various tumor cell lines.

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Novel pyrazole analogues show promising antibacterial, antifungal, and anti-inflammatory properties, warranting further development of new antibacterial, antifungal, and anti-inflammatory drugs.

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Compound 4 with sulphonamide derivative is the most potent pyrazole-3-one derivative for hypoglycemic activity in diabetic rats, based on docking studies and in vivo tests.

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Microwave-assisted synthesis of novel pyrazole derivatives led to compounds with maximum anti-inflammatory and analgesic activities compared to Diclofenac sodium.

Citations

Synthesis, anti-inflammatory properties, molecular modelling and potential COX-2, TNF-α, PGE2 and IL1β inhibitors of pyrazole-based scaffolds

Compound 8 shows the best anti-inflammatory properties, antipyretic effect, and long-lasting analgesic activity without ulcerogenic potential, making it a promising candidate for developing into an anti-inflammatory drug.

Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities

Benzimidazole-pyrazole hybrids show promising antimicrobial properties and potential pharmaceutical applications in the COVID-19 pandemic.

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The synthesized fluorinated pyrazole shows a close binding affinity to human estrogen alpha receptor, with potential applications in pharmaceuticals and cosmetics.

SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL 3,4-DISUBSTITUTED PYRAZOLE DERIVATIVES

The developed 3,4-substituted pyrazole derivatives show significant antibacterial properties and antifungal properties, suggesting potential as lead structures for developing antimicrobial agents for fatal infections.