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RESEARCH PRODUCT

Synthesis and anti-inflammatory activity of chalcone derivatives

M.luisa FerrándizM. José AlcarazJaime CharrisAmalia UbedaGricela LoboJosén. DomínguezFelipe Herencia

subject

ChalconeNeutrophilsmedicine.drug_classLeukotriene B4Clinical BiochemistryPharmaceutical ScienceLeukotriene B4BiochemistryChemical synthesisAnti-inflammatoryMiceStructure-Activity Relationshipchemistry.chemical_compoundChalconeIn vivoDrug DiscoverymedicineAnimalsHumansCyclooxygenase InhibitorsLipoxygenase InhibitorsMolecular BiologyPropiophenonesArachidonate 5-LipoxygenaseCyclooxygenase 2 InhibitorsMolecular StructureChemistrySuperoxideAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryDegranulationMembrane ProteinsIn vitroIsoenzymesBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesDrug DesignMolecular Medicine

description

Chalcones and their derivatives were synthesized and evaluated for their anti-inflammatory activity. In vitro, chalcones 2, 4, 8, 10 and 13 inhibited degranulation and 5-lipoxygenase in human neutrophils, whereas 11 behaved as scavenger of superoxide. Only four compounds (4-7) inhibited cyclo-oxygenase-2 activity. The majority of these samples showed anti-inflammatory effects in the mouse air pouch model.

https://doi.org/10.1016/s0960-894x(98)00179-6