6533b871fe1ef96bd12d1b1b
RESEARCH PRODUCT
6-Dimethylamino 1H-pyrazolo[3,4-d]pyrimidine derivatives as new inhibitors of inflammatory mediators in intact cells.
M.luisa FerrándizRicardo RigueraCarlos PeinadorIsabel DevesaJosé M. QuintelaL. GonzalezMaría José Alcarazsubject
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 Mediatorsdescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2003-03-01 | Bioorganicmedicinal chemistry |