SYNTHESIS AND EVALUATION OF 1, 3, 4-OXADIAZOLE SUBSTITUTED DICLOFENAC ACID: ANTI-INFLAMMATORY ACTIVITY WITH REDUCED ULCEROGENICITY
Radha Sharma, Divya Yadav, Divya Gumber, Karuna Pandey, Rakesh Yadav*, Anurag Kuhad and
Satyender K. Yadav
ABSTRACT
Background: A new series of 1,3,4-oxadiazole substituted diclofenac acid derivatives has been synthesized and
evaluated in vivo for anti-inflammatory activity and ulcerogenic effects. It was observed that the nature of
substituent at carboxyl group on the diclofenac moiety remarkably affects the anti-inflammatory activity and
ulceration index. In the present paper, the results of synthesis and pharmacological findings of a series of Schiff
bases of 1, 3, 4-oxadiazole substituted diclofenac acid are described. Both, the moieties are important due to their
versatile biological actions. Findings: The present work encompasses the functionalization of oxadiazole system
onto the diclofenac acid moiety for the synthesis of various compounds. The structures of the newly synthesized
compounds were characterized by TLC, FT-IR, 1H-NMR and elemental analysis. The compounds were also tested
in vivo for their anti-inflammatory activity and ulcerogenicity index. Among the synthesized derivatives 6a-g, 6c
was found to be most active in comparison to the standard. Conclusion: Synthesized and recorded antiinflammatory
and ulcerogenicity activity of some new 1,3,4-oxadiazole substituted diclofenac acid derivatives.
Keywords: NSAIDs, Diclofenac Acid, Oxadiazole, Carrageenan.
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