Synthesis and evaluation of 2-tosylamino and 2-tosyliminopyrimidine derivatives as inhibitors of some leukocyte functions.
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.
Fernandez-Ferri
Patricia
P
Departamento de Farmacologi;a, Universitat de Valencia, 46100, Burjassot, Spain.
Ubeda
Amalia
A
Guillén
Isabel
I
Lasri
Jamal
J
González-Rosende
M Eugenia
ME
Akssira
Mohamed
M
Sepúlveda-Arques
José
J
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*
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