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

Franco Heidempergher, Paolo Pevarello, Antonio Pillan, Vittorio Pinciroli, Arturo Della Torre, Carmela Speciale, Marina Marconi, Massimo Cini, Salvatore Toma, Felicita Greco, Mario Varasi

Research output: Contribution to journalArticle

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 (KYN3-OHase). A molecular modelling study showed a good superimposition of 7a with PNU-156561 and kynurenine the natural substrate of KYN-3-OHase.

Original languageEnglish
Pages (from-to)152-160
Number of pages9
JournalFarmaco, Edizione Pratica
Volume54
Issue number3
DOIs
Publication statusPublished - Mar 31 1999

Keywords

  • Enzyme inhibition
  • Hydroxylase
  • Kynurenine

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmaceutical Science

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