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

页码：1619 / 1624

页数：6

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