6533b7d3fe1ef96bd125ff8c
RESEARCH PRODUCT
Synthesis and inhibitory activity of dimethylamino-chalcone derivatives on the induction of nitric oxide synthase.
Jaime CharrisJose N. DominguezJavier RojasGricela LoboM.luisa FerrándizMiguel Payásubject
ChalconeAnti-Inflammatory AgentsDrug Evaluation PreclinicalAdministration OralNitric Oxide Synthase Type IIInflammationInhibitory postsynaptic potentialChemical synthesisDinoprostoneNitric oxideCell Linechemistry.chemical_compoundMiceStructure-Activity RelationshipChalconeWestern blotDrug DiscoverymedicineOral routeAnimalsEdemaPharmacologychemistry.chemical_classificationmedicine.diagnostic_testbiologyMacrophagesOrganic ChemistryDual inhibitorMacrophage cellGeneral MedicineMolecular biologyNitric oxide synthaseEnzymeBiochemistrychemistryEnzyme inhibitorCell cultureEnzyme Inductionbiology.proteinmedicine.symptomNitric Oxide SynthaseDimethylaminesdescription
A series of nine dimethylamino-chalcone derivatives (1,3-diaryl-propenones) was synthesized and screened as potential inhibitors of NO and PGE(2) production in the RAW 264.7 macrophage cell line. 4-Dimethylamino-2',5'-dimethoxychalcone (6) was found to be the most potent and dual inhibitor (IC(50s) in the submicromolar range) of NO and PGE(2) production. 2',6'-Dimethoxylation appeared to be an effective requirement for selective and potent inhibition of nitric oxide synthase induction as it was confirmed by Western blot analysis. Chalcone (6) at 25 mg kg(-1) by oral route, inhibited significantly the formation of oedema in the carrageenan-induced model of inflammation in mice.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2002-08-06 | European journal of medicinal chemistry |