Journal of Enzyme Inhibition and Medicinal Chemistry · 2003 · 334 citations · 2 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryInflammationStructure-activity RelationshipsAnti-inflammatory PharmacologyInflammation PharmacologyInflammatory ArthritisMedicinal PlantsReactive Oxygen SpeciesStructure-activity Relationship AnalysisActivitiesAnti-inflammatory ActivityAnti-inflammatory MechanismsAnti-inflammatory Natural ProductsAnti-inflammatory ResponseAntioxidant PharmacologyBiological Evaluation Report
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.
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C. Bezergiannidou‐Balouctsi, Konstantions E. Litians, Elizabeth Malamidou‐Xenikaki et al. · Liebigs Annalen der Chemie · 1993 · 17 citations