title: Synthesis and evaluation of 2-tosylamino and 2-tosyliminopyrimidine derivatives as inhibitors of some leukocyte functions.
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 microM 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.
authors.affiliation: Departamento de Farmacologi;a, Universitat de Valencia, 46100, Burjassot, Spain.
authors.forename: Patricia
authors.initials: P
authors.lastname: Fernandez-Ferri
authors.forename: Amalia
authors.initials: A
authors.lastname: Ubeda
authors.forename: Isabel
authors.initials: I
authors.lastname: Guillén
authors.forename: Jamal
authors.initials: J
authors.lastname: Lasri
authors.forename: M Eugenia
authors.initials: ME
authors.lastname: González-Rosende
authors.forename: Mohamed
authors.initials: M
authors.lastname: Akssira
authors.forename: José
authors.initials: J
authors.lastname: Sepúlveda-Arques
mesh_terms: D001094:Arachidonate 5-Lipoxygenase / Q000378:metabolism; D015550:Cell Degranulation / Q000187:drug effects; D002469:Cell Separation; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D019272:Leukocyte Elastase / Q000378:metabolism; D007962:Leukocytes / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D007975:Leukotriene B4 / Q000096:biosynthesis; D016859:Lipoxygenase Inhibitors; D009682:Magnetic Resonance Spectroscopy; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D014105:Tosyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: C479502:2-tosyliminopyrimidine; D007202:Indicators and Reagents; D016859:Lipoxygenase Inhibitors; D011743:Pyrimidines; D014105:Tosyl Compounds; D007975:Leukotriene B4; D001094:Arachidonate 5-Lipoxygenase; D019272:Leukocyte Elastase