Piperazinyl oxime ethers as NK-1 receptor antagonists

被引:2
作者
van den Hoogenband, A [1 ]
van Maarseveen, JH [1 ]
McCreary, AC [1 ]
Mulder, AT [1 ]
van Scharrenburg, GJM [1 ]
van Stuivenberg, HH [1 ]
Zethof, TJJ [1 ]
Zijta, B [1 ]
Bakker, WII [1 ]
机构
[1] Solvay Pharmaceut, Res Labs, NL-1381 CP Weesp, Netherlands
关键词
neurokinin; synthesis; SAR; oxime ethers;
D O I
10.1016/j.bmcl.2005.10.077
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and structure-activity relations for a new class of centrally active NK-1 receptor antagonists are described. The new compounds are based on piperazine 2 and contain an oxime ether functionality. Several new compounds have high affinity for the NK-1 receptor and show good antagonistic activity in the gerbil foot-tapping assay. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1045 / 1048
页数:4
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