S-aryl cysteine S,S-dioxides as inhibitors of mammalian kynureninase.
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.
Drysdale
M J
MJ
Glaxo Wellcome Research and Development, Stevenage, Hertfordshire, UK. MJD30029@ggr.co.uk
Reinhard
J F
JF
D002478:Cells, Cultured; D003545:Cysteine / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006867:Hydrolases / Q000037:antagonists & inhibitors*; D008264:Macrophages / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D017378:Quinolinic Acid / Q000378:metabolism
D004791:Enzyme Inhibitors; D006867:Hydrolases; C021480:kynureninase; D017378:Quinolinic Acid; D003545:Cysteine