Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles:: Potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors

被引：6
|
作者：
Tamiz, AP
Whittemore, ER
Woodward, RM
Upasani, RB
Keana, JFW
机构：
[1] CoCensys Inc, Irvine, CA 92618 USA
[2] Univ Oregon, Dept Chem, Eugene, OR 97403 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 11期
关键词：
D O I：
10.1016/S0960-894X(99)00248-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b] indoles was synthesized as potential antagonists for the NR1A/2B subtype of N-methyl-D-aspartate (NMDA) receptors. Assayed by electrical recording under steady-state conditions, 7-hydroxy-2-(4-phenylbutyl)-1,2,3,4-tetrahydropyrido-[3,4-b]indole (30) was the most potent compound in the series having an IC50 value of 50 nM at the MR1A/2B receptors. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1619 / 1624
页数：6
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