S-aryl cysteine S,S-dioxides as inhibitors of mammalian kynureninase

Bioorg Med Chem Lett. 1998 Jan 20;8(2):133-8. doi: 10.1016/s0960-894x(97)10209-8.

Abstract

A series of 2-amino-S-aryl cysteine S,S-dioxides have been synthesised and shown to inhibit kynureninase an important enzyme in the biosynthesis of the known excitotoxic moiety quinolinic acid. The most potent of these, 2-amino-5-methyl-S-phenyl cysteine S,S-dioxide 6d, inhibits interferon-gamma induced synthesis of quinolinic acid in human macrophages.

MeSH terms

  • Cells, Cultured
  • Cysteine / pharmacology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Hydrolases / antagonists & inhibitors*
  • Macrophages / drug effects
  • Macrophages / enzymology
  • Macrophages / metabolism
  • Quinolinic Acid / metabolism

Substances

  • Enzyme Inhibitors
  • Hydrolases
  • kynureninase
  • Quinolinic Acid
  • Cysteine