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

被引：23

作者：

Heidempergher, F ^{[1
]}

Pevarello, P ^{[1
]}

Pillan, A ^{[1
]}

Pinciroli, V ^{[1
]}

Della Torre, A ^{[1
]}

Speciale, C ^{[1
]}

Marconi, M ^{[1
]}

Cini, M ^{[1
]}

Toma, S ^{[1
]}

Greco, F ^{[1
]}

Varasi, M ^{[1
]}

机构：

[1] Pharmacia & Upjohn Inc, Dept Chem, I-20014 Milan, Italy

来源：

FARMACO | 1999年 / 54卷 / 03期

关键词：

kynurenine; hydroxylase; enzyme inhibition;

D O I：

10.1016/S0014-827X(99)00009-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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. (C) 1999 Elsevier Science S.A. All rights reserved.

引用

页码：152 / 160

页数：9

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