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

Authors
Heidempergher, F Pevarello, P Pillan, A Pinciroli, V Della Torre, A Speciale, C Marconi, M Cini, M Toma, S Greco, F Varasi, M
Citation
F. Heidempergher et al., Pyrrolo[3,2-c]quinoline derivatives: a new class of kynurenine-3-hydroxylase inhibitors, FARMACO, 54(3), 1999, pp. 152-160
Citations number
21
Categorie Soggetti
Pharmacology & Toxicology
Journal title
FARMACO
ISSN journal
0014827X → ACNP
Volume
54
Issue
3
Year of publication
1999
Pages
152 - 160
Database
ISI
SICI code
0014-827X(19990331)54:3<152:PDANCO>2.0.ZU;2-X
Abstract
A series of pyrrolo[3,2-c]quinoline derivatives were synthesised and evalua ted 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. (C) 19 99 Elsevier Science S.A. All rights reserved.