Pyrrolo[3,2-c]quinoline derivatives: a new class of kynurenine-3-hydroxylase inhibitors. |
| |
| Authors: | F Heidempergher P Pevarello A Pillan V Pinciroli A Della Torre C Speciale M Marconi M Cini S Toma F Greco M Varasi |
| |
| Affiliation: | Pharmacia & Upjohn, Chemistry Department, Milan, Italy. |
| |
| 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. |
| |
| Keywords: | |
|
|
