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4,5-Dihydro-1H-Pyrazole-1-Carbaldehyde: Synthesis, Anti-Inflammatory Activity and Docking Study
Published:
03 November 2014
by MDPI
in The 18th International Electronic Conference on Synthetic Organic Chemistry
session Computational Chemistry
Abstract: A series of 3-phenyl-5-aryl-4,5-dihydro-1H-pyrazole-1-carbaldehyde 4(a-j) was prepared by heating chalcones 3(a-j) and hydrazine hydrate in presence of formic acid. The synthesized compounds were investigated for in-vivo anti-inflammatory activity in Carrageenan induced rat paw edema model. Some of the synthesized derivatives exhibited good anti-inflammatory activity as compared to diclofenac, while some derivatives have shown comparable anti-inflammatory activity to that of diclofenac. All the synthesized derivatives were found to be potent anti-inflammatory agents. Some of the derivatives were evaluated for ulcerogenic potential and their ulcer index was found to be less than the standard drug diclofenac. The molecular docking analysis was performed to understand the binding interactions of these compounds to COX-2 enzyme. The results from the present investigation suggests that 3-phenyl-5-aryl-4, 5-dihydro-1H-pyrazole-1-carbaldehyde as a promising template for the design of new anti-inflammatory agents.
Keywords: Pyrazole carbaldehyde; anti-inflammatory; NSAIDs; rat paw edema; molecular docking