Abstract

Synthesis, Characterization and Evaluation of Analgesic, Anti-Inflammatory, Ulcerogenic Potential of Some 2-Pyrazoline Derivatives

Author(s): B. Dipankar, P. Panneerselvam and B. Asish

The discovery of cyclooxygenase-2, expressed in response to inflammatory stimuli, present in the central nervous system, not in the gastric mucosa has provided a unique opportunity in the development of NSAIDs that lack the ulcerogenic effect. Thus it has led to the hypothesis that selective inhibitor of COX-2 over COX-1 may be better antiinflammatory agent with less adverse effects than the classical NSAIDs. As classical NSAIDs like aspirin, indomethacin are nonselective with respect two both isoforms. The preferential binding affinity of classical NSAIDs to COX-1 leads to mechanism based gastrointestinal, renal, hepatic side effects. Two varieties of acetophenones were condensed with three varieties of substituted benzaldehyde derivatives to get six chalcone derivatives which undergo condensation followed by cyclisation with isoniazid and 1-(2-napthyloxy acetate) hydrazine two get the final twelve 2-pyrazoline derivatives. The synthesized compounds were characterized by IR, 1H-NMR and mass spectral studies. The synthesized compounds were evaluated for their analgesic and anti-inflammatory activity. Two compounds which exhibited comparatively better analgesic and anti-inflammatory activity among the synthesized derivatives were screened for their ulcerogenic potential and were found to be less ulcerogenic than the standard diclofenac sodium.

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