Synthesis and evaluation of 2-tosylamino and 2-tosyliminopyrimidine derivatives as inhibitors of some leukocyte functions

Eur J Med Chem. 2003 Mar;38(3):289-96. doi: 10.1016/s0223-5234(03)00013-8.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arachidonate 5-Lipoxygenase / metabolism
  • Cell Degranulation / drug effects
  • Cell Separation
  • Humans
  • In Vitro Techniques
  • Indicators and Reagents
  • Leukocyte Elastase / metabolism
  • Leukocytes / drug effects*
  • Leukocytes / metabolism
  • Leukocytes / ultrastructure
  • Leukotriene B4 / biosynthesis
  • Lipoxygenase Inhibitors
  • Magnetic Resonance Spectroscopy
  • Neutrophils / drug effects
  • Neutrophils / metabolism
  • Neutrophils / ultrastructure
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology*
  • Tosyl Compounds / chemical synthesis*
  • Tosyl Compounds / pharmacology*

Substances

  • 2-tosyliminopyrimidine
  • Indicators and Reagents
  • Lipoxygenase Inhibitors
  • Pyrimidines
  • Tosyl Compounds
  • Leukotriene B4
  • Arachidonate 5-Lipoxygenase
  • Leukocyte Elastase