Quinoline-2,4-dicarboxylic acids: Synthesis and evaluation as inhibitors of the glutamate vesicular transport system

被引：31

作者：

Carrigan, CN

Esslinger, CS

Bartlett, RD

Bridges, RJ

Thompson, CM ^{[1
]}

机构：

[1] Univ Montana, Dept Pharmaceut Sci, Missoula, MT 59812 USA

[2] Univ Montana, Dept Chem, Missoula, MT 59812 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(99)00444-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Twenty-six quinoline-2,4-dicarboxylic acids (QDC's) were synthesized by a modified Doebner-von Miller pathway and tested as inhibitors against the glutamate vesicular transport (GVT) protein. The QDC's were active as inhibitors with the most potent QDC's found to contain halogens at the 6-/8-position, a hydroxyl at the 8-position, or a tethered aromatic moiety at the 6- or 7-position of the quinoline. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2607 / 2612

页数：6

共 12 条

[1] Substituted quinolines as inhibitors of L-glutamate transport into synaptic vesicles [J].