Structure-activity relationship of thiopyrimidines as mGluR5 antagonists

被引:12
作者
Hammerland, LG
Johansson, M
Malmström, J
Mattsson, JP
Minidis, ABE [1 ]
Nilsson, K
Peterson, A
Wensbo, D
Wållberg, A
Österlund, K
机构
[1] Astra Zeneca R&D Sodertalje, Local Discovery CNS & Pain Control, Med Chem, SE-15185 Sodertalje, Sweden
[2] NPS Pharmaceut, Salt Lake City, UT 84108 USA
[3] Astra Zeneca R&D Molndal, Med Chem, SE-43183 Molndal, Sweden
关键词
thiopyrimidine; metabotropic glutamate receptor; mGluR5;
D O I
10.1016/j.bmcl.2006.01.100
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Structure-activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity. (C) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2467 / 2469
页数:3
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