6533b830fe1ef96bd12967b5
RESEARCH PRODUCT
Synthesis and evaluation of 2-tosylamino and 2-tosyliminopyrimidine derivatives as inhibitors of some leukocyte functions
Patricia Fernandez-ferriM. Eugenia González-rosendeAmalia UbedaIsabel GuillénMohamed AkssiraJamal LasriJosé Sepúlveda-arquessubject
Magnetic Resonance SpectroscopyNeutrophilsLeukotriene B4Inflammatory responseCell SeparationIn Vitro TechniquesLeukotriene B4Cell DegranulationTosyl Compounds2-tosyliminopyrimidinechemistry.chemical_compoundLipoxygenaseBiosynthesisDrug DiscoveryLeukocytesHumansLipoxygenase InhibitorsPharmacologychemistry.chemical_classificationArachidonate 5-LipoxygenasebiologyChemistryOrganic ChemistryElastaseGeneral MedicineIn vitroPyrimidinesEnzymeBiochemistryEnzyme inhibitorArachidonate 5-lipoxygenaseLeukotriene Bbiology.proteinNeutrophil degranulationIndicators and ReagentsLeukocyte Elastasedescription
Abstract We have studied the potential anti-inflammatory effects of 20 2-tosylamino and 2-tosyliminopyrimidine new derivatives in human neutrophils. We have evaluated their interference with some leukocyte functions and 5-lipoxygenase activity. All the compounds reduced neutrophil degranulation process at concentrations in the μM range. Besides, compounds with a phenolic substitution inhibited leukotriene B 4 biosynthesis in neutrophils and decreased the cell-free 5-lipoxygenase activity. This study demonstrates that 2-tosylamino and 2-tosyliminopyrimidine derivatives can reduce the activation of neutrophil cells which may have relevance for the modulation of the inflammatory response.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2003-08-05 | European Journal of Medicinal Chemistry |