0000000001053853

AUTHOR

L. Gonzalez

showing 2 related works from this author

An anti-inflammatory ditriazine inhibiting leukocyte functions and expression of inducible nitric oxide synthase and cyclo-oxygenase-2.

2000

A ditriazine derivative (4,10-dichloropyrido[5,6:4,5]thieno[3,2-d':3, 2-d]-1,2,3-ditriazine (DTD)) inhibited neutrophil functions, including degranulation, superoxide generation, and leukotriene B(4) production, without any effect on 5-lipoxygenase activity. This compound reduced nitric oxide (NO) and prostaglandin E(2) production in mouse peritoneal macrophages stimulated with lipopolysaccharide, whereas no influence on the activity of inducible NO synthase, cyclo-oxygenase-2 or cyclo-oxygenase-1 was observed. DTD significantly reduced mouse paw oedema induced by carrageenan and also markedly reduced NO and prostaglandin E(2) levels in exudates from 24-h zymosan-stimulated mouse air pouch.…

LipopolysaccharideLeukotriene B4Neutrophilsmedicine.medical_treatmentAnti-Inflammatory AgentsNitric Oxide Synthase Type IICarrageenanNeutrophil Activationchemistry.chemical_compoundMiceLeukocytesEdemaProstaglandin E2biologyPancreatic ElastaseSuperoxideTriazinesHindlimbNitric oxide synthaseIsoenzymesBiochemistryFemalemedicine.drugProstaglandin EBlood PlateletsLeukotriene B4DinoprostonePhospholipases ANitric oxideMicrosomesmedicineAnimalsHumansNitritesPharmacologyInflammationCell-Free SystemDose-Response Relationship DrugZymosanMembrane ProteinsMolecular biologyThromboxane B2chemistryEicosanoidCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesLuminescent Measurementsbiology.proteinMacrophages PeritonealNitric Oxide SynthaseEuropean journal of pharmacology
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6-Dimethylamino 1H-pyrazolo[3,4-d]pyrimidine derivatives as new inhibitors of inflammatory mediators in intact cells.

2003

The synthesis of 6-dimethylamino 1H-pyrazolo[3,4-d]pyrimidines substituted at positions 1 and 4, and their effects on murine macrophage and human neutrophil functions are described. Several compounds and especially 4b-6b are potent inhibitors of PGE2 generation in murine macrophages. This action is related to a direct effect on COX-2 activity without affecting the enzyme expression. Some of these compounds also inhibited COX-1 and COX-2 in human monocytes and 4b showed selectivity for COX-2 inhibition. © 2003 Elsevier Science Ltd. All rights reserved.

LipopolysaccharidesMagnetic Resonance SpectroscopyPyrimidineClinical BiochemistryBlotting WesternPharmaceutical ScienceBiochemistryLeukotriene B4Pyrazolopyrimidinechemistry.chemical_compoundMiceStructure-Activity RelationshipDrug DiscoverymedicineLeukocytesMacrophageAnimalsHumansCyclooxygenase InhibitorsMolecular Biologychemistry.chemical_classificationbiologyCyclooxygenase 2 InhibitorsPancreatic ElastaseMonocyteOrganic ChemistryMembrane ProteinsBiological activityIn vitroIsoenzymesEnzymemedicine.anatomical_structurePyrimidineschemistryBiochemistryEnzyme inhibitorCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesLuminescent Measurementsbiology.proteinCyclooxygenase 1Macrophages PeritonealMolecular MedicinePyrazolesInflammation MediatorsBioorganicmedicinal chemistry
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