Design, synthesis and evaluation of antiinflammatory, analgesic and ulcerogenicity studies of novel S-substituted phenacyl-1,3,4-oxadiazole-2-thiol and Schiff bases of diclofenac acid as nonulcerogenic derivatives.

摘要: Abstract Diclofenac sodium is being used for its anti-inflammatory actions since 28 years, but as all the NSAIDs are suffering from deadlier GI toxicities, diclofenac also not an exception to these toxicities. The free –COOH group thought be responsible toxicity associated with traditional NSAIDs. In present research work, main motto was develop new chemical entities potential agents no this paper, results of synthesis and pharmacological screening a series S-substituted phenacyl 1,3,4-oxadiazoles Schiff bases derived 2-[(2,6-dichloroanilino) phenyl] acetic acid (diclofenac acid) described. moieties important because their versatile biological actions. studies, oxadiazole system has been functionalized onto moiety 18 compounds in were synthesized. structures characterized by TLC, FTIR, 1H NMR Mass spectral data. These tested vivo activity. compounds, which showed significant activity (comparable standard drug sodium), screened analgesic check ability induce ulcers ulcerogenicity histopathology studies. Eight out 18, found have carrageenan induced rat paw oedema model, writhing model ulcerogenicity. negligible ulcerogenic action, promising that is, they causing mucosal injury.