Substituted morpholine-2S-acetic acid derivatives: Sch 50911 and related compounds as novel GABA(B) antagonists

被引:19
作者
Blythin, DJ [1 ]
Kuo, SC [1 ]
Shue, HJ [1 ]
McPhail, AT [1 ]
Chapman, RW [1 ]
Kreutner, W [1 ]
Rizzo, C [1 ]
She, HS [1 ]
West, R [1 ]
机构
[1] DUKE UNIV,PAUL M GROSS CHEM LAB,DURHAM,NC 27708
关键词
D O I
10.1016/S0960-894X(96)00267-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and GABA(B) antagonist activity of a series of substituted morpholine-2-acetic acid derivatives is described. Resolution of the lead compound from the series produces one active and one inactive enantiomer. X-ray analysis of a halogenated derivative (25) of the active enantiomer Sch 50911 (23) shows that it possesses the 2S configuration. Copyright (C) 1996 Elsevier Science Ltd
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收藏
页码:1529 / 1534
页数:6
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