New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects

被引：51

作者：

Kamei, K

Maeda, N

Ogino, R

Koyama, M

Nakajima, M

Tatsuoka, T

Ohno, T

Inoue, T

机构：

[1] Suntory Biomed Res Ltd, Shimamoto, Osaka 6188503, Japan

[2] Suntory Ltd, Chiyoda Ku, Tokyo 1028530, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)00008-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new 3-substituted-4-(4-aminobutyl)-1,4-benzoxazepin-5(4H)-one derivatives (1-5) which showed a very high affinity for 5-HT1A receptor with good selectivity over dopamine D-2 receptor was synthesized. Among these compounds, 3-chloro4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]-1,4-benzoxazepin-5(4H)-one (5. SUN N4057) exhibited remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：595 / 598

页数：4

共 25 条

[1] SELECTIVE DOPAMINE-D2 ANTAGONIST AND PROLACTIN RESPONSE IN ACUTE SCHIZOPHRENIA - RESULTS FROM REMOXIPRIDE STUDIES [J].