title: Pyrrolo[3,2-c]quinoline derivatives: a new class of kynurenine-3-hydroxylase inhibitors.
abstract: A series of pyrrolo[3,2-c]quinoline derivatives were synthesised and evaluated as inhibitors of selected enzymes of the kynurenine pathway. 7-Chloro-3-methyl-1H-pyrrolo[3,2-c]quinoline-4-carboxylic acid (7a) was found to be a relatively potent and selective inhibitor of kynurenine-3-hydroxylase (KYN-3-OHase). A molecular modelling study showed a good superimposition of 7a with PNU-156561 and kynurenine the natural substrate of KYN-3-OHase.
authors.affiliation: Pharmacia & Upjohn, Chemistry Department, Milan, Italy.
authors.forename: F
authors.initials: F
authors.lastname: Heidempergher
authors.forename: P
authors.initials: P
authors.lastname: Pevarello
authors.forename: A
authors.initials: A
authors.lastname: Pillan
authors.forename: V
authors.initials: V
authors.lastname: Pinciroli
authors.forename: A
authors.initials: A
authors.lastname: Della Torre
authors.forename: C
authors.initials: C
authors.lastname: Speciale
authors.forename: M
authors.initials: M
authors.lastname: Marconi
authors.forename: M
authors.initials: M
authors.lastname: Cini
authors.forename: S
authors.initials: S
authors.lastname: Toma
authors.forename: F
authors.initials: F
authors.lastname: Greco
authors.forename: M
authors.initials: M
authors.lastname: Varasi
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D050601:Kynurenine 3-Monooxygenase; D008099:Liver / Q000201:enzymology; D006899:Mixed Function Oxygenases / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
chemical_list: C120225:7-chloro-3-methyl-1H-pyrrolo(3,2-c)quinoline-4-carboxylic acid; D004791:Enzyme Inhibitors; D011758:Pyrroles; D011804:Quinolines; D006899:Mixed Function Oxygenases; D050601:Kynurenine 3-Monooxygenase