Identification of a series of 1,2,3,4-tetrahydroisoquinolinyl-benzamides with potential anticonvulsant activity

被引:9
作者
Chan, WN [1 ]
Hadley, MS [1 ]
Harling, JD [1 ]
Herdon, HJ [1 ]
Jerman, JC [1 ]
Orlek, BS [1 ]
Stean, TO [1 ]
Thompson, M [1 ]
Upton, N [1 ]
Ward, RW [1 ]
机构
[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England
关键词
anticonvulsant activity; molecular modelling; heterocyclic compounds; SB-204269 binding site;
D O I
10.1016/S0960-894X(98)00523-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of N-(tetrahydroisoquinolinyl)-2-methoxybenzamides was identified by high-throughput screening at the novel SE-204269 binding site. SAR studies have provided compounds 4 and 14 with high affinity and good anticonvulsant activity in animal models. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2903 / 2906
页数:4
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