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

F Heidempergher, P Pevarello, A Pillan, V Pinciroli…

Index: Heidempergher, Franco; Pevarello, Paolo; Pillan, Antonio; Pinciroli, Vittorio; Della Torre, Arturo; Speciale, Carmela; Marconi, Marina; Cini, Massimo; Toma, Salvatore; Greco, Felicita; Varasi, Mario Farmaco, 1999 , vol. 54, # 3 p. 152 - 160

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Citation Number: 15

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 ...