Pyrrolo[3,2- c]quinoline derivatives: a new class of kynurenine-3-hydroxylase inhibitors

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-1 H-pyrrolo[3,2- c]quinoline-4-carboxylic acid ( 7a) was found to be a relatively potent and selective inhibitor of kynurenine-3-hydroxylase...

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Veröffentlicht in:	Farmaco (Società chimica italiana : 1989) 1999-03, Vol.54 (3), p.152-160
Hauptverfasser:	Heidempergher, Franco, Pevarello, Paolo, Pillan, Antonio, Pinciroli, Vittorio, Della Torre, Arturo, Speciale, Carmela, Marconi, Marina, Cini, Massimo, Toma, Salvatore, Greco, Felicita, Varasi, Mario
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Enzyme inhibition Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Hydroxylase Kynurenine Kynurenine 3-Monooxygenase Liver - enzymology Medical sciences Miscellaneous Mixed Function Oxygenases - antagonists & inhibitors Molecular Structure Neuropharmacology Pharmacology. Drug treatments Pyrroles - chemical synthesis Pyrroles - pharmacology Quinolines - chemical synthesis Quinolines - pharmacology Rats
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Zusammenfassung:	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-1 H-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.
ISSN:	0014-827X 1879-0569
DOI:	10.1016/S0014-827X(99)00009-9