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New diaminoether coumarinic derivatives with anti-inflammatory activity
1Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece. hadjipav@pharm.auth.gr
Abstract:
Four coumarinyl-oxy-diamines were synthesized and tested as anti-inflammatory agents. pKa and log P were theoretically calculated. These compounds were tested for their ability to interact with 1,1-diphenyl-2-picrylhydrazyl stable free radical (DPPH), to inhibit proteolysis and soybean lipoxygenase (LOX) in vitro. They were found to inhibit proteolysis (82-90%) and soybean lipoxygenase activity (52-79%) very significant. On the contrary, their reducing ability was found to be low (8-22%). The effect of the synthesised compounds on inflammation using the carageenan-induced rat paw oedema model was studied. They showed a potent inhibitory effect on inflammation (37-55%). Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesised compounds.