Abstract
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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