Abstract
With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.
Keywords:
1,3-diaryl pyrazole derivatives; anti-inflammatory activity; synthesis.
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Anti-Inflammatory Agents / therapeutic use
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Carrageenan
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Celecoxib / chemistry
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Celecoxib / pharmacology
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Cyclooxygenase Inhibitors / therapeutic use
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Drug Design*
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Edema / chemically induced
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Edema / drug therapy
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Heterocyclic Compounds / chemical synthesis*
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacology*
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Heterocyclic Compounds / therapeutic use
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Injections
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Male
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Molecular Docking Simulation
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Piperidines / chemistry
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Piperidines / pharmacology
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Pyrazoles / therapeutic use
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Rats
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Rimonabant
Substances
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Anti-Inflammatory Agents
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Cyclooxygenase Inhibitors
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Heterocyclic Compounds
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Piperidines
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Pyrazoles
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pyrazole
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Carrageenan
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Celecoxib
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Rimonabant