Biological evaluation of several coumarin derivatives designed as possible anti-inflammatory/antioxidant agents.
Several linear and angular coumarins designed and synthesised as possible anti-inflammatory and antioxidant agents were evaluated for their biological activities, using the carrageenin-induced rat paw oedema model. In general, the compounds were found to be potent anti-inflammatory agents. Compound (4) was found to possess protective properties in adjuvant-induced arthritis in rats. The compounds were found to interact with 1,1-diphenyl-2-picryl-hydrazyl stable free radical (DPPH) whereas most of them were essentially inactive in other tests. The anti-inflammatory activity seemed to be connected with their reducing activity. R(M) values were determined as an expression of their lipophilicity which was also calculated as clog P. Only a poor relationship existed between lipophilicity and anti-inflammatory activity.
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.
Christos
C
Kontogiorgis
Dimitra
D
Hadjipavlou-Litina
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D003374:Coumarins / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D051381:Rats; D011916:Rats, Inbred F344
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D003374:Coumarins; C030123:coumarin