5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5. doi: 10.1016/j.bmcl.2004.12.023.

Abstract

A series of N-hydroxycarbamates containing a histaminergic H(1) receptor antagonist pharmacophore was synthesized. In vitro assays determined the compounds had both histaminergic binding and 5-lipoxygenase inhibiting activities comparable to the corresponding N-hydroxyurea analog. Animal models demonstrated antihistaminergic and the 5-lipopxygenase inhibitory activity, with the N-hydroxyurea analog having a better overall profile.

MeSH terms

  • Animals
  • Blood
  • Guinea Pigs
  • Histamine H1 Antagonists / chemical synthesis
  • Histamine H1 Antagonists / chemistry
  • Humans
  • Hydroxamic Acids / chemical synthesis*
  • Hydroxamic Acids / pharmacology
  • Inhibitory Concentration 50
  • Leukotriene B4 / biosynthesis
  • Lipoxygenase Inhibitors*
  • Protein Binding
  • Structure-Activity Relationship

Substances

  • Histamine H1 Antagonists
  • Hydroxamic Acids
  • Lipoxygenase Inhibitors
  • Leukotriene B4