title: S-aryl cysteine S,S-dioxides as inhibitors of mammalian kynureninase.
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.
authors.affiliation: Glaxo Wellcome Research and Development, Stevenage, Hertfordshire, UK. MJD30029@ggr.co.uk
authors.forename: M J
authors.initials: MJ
authors.lastname: Drysdale
authors.forename: J F
authors.initials: JF
authors.lastname: Reinhard
mesh_terms: 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
chemical_list: D004791:Enzyme Inhibitors; D006867:Hydrolases; C021480:kynureninase; D017378:Quinolinic Acid; D003545:Cysteine