Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry

被引：39
|
作者：
Corbett, DF
Heightman, TD
Moss, SF
Bromidge, SM
Coggon, SA
Longley, MJ
Roa, AM
Williams, JA
Thomas, DR
机构：
[1] GlaxoSmithKline Inc, Discovery Res, High Throughput Chem, Harlow CM19 5AW, Essex, England
[2] GlaxoSmithKline Inc, Neurol & GI Ctr Excellence Drug Discovery, Harlow CM19 5AW, Essex, England
[3] GlaxoSmithKline Inc, Psychiat Ctr Excellence Drug Discovery, Harlow CM19 5AW, Essex, England
[4] Glaxo SmithKline Pharmaceut, Screening Sci Dept, Ctr Invest Basica, Madrid 28760, Spain
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 18期
关键词：
5-ht(5A) receptor; 5-ht(5A) antagonist; high-throughput chemistry; solid-phase synthesis;
D O I：
10.1016/j.bmcl.2005.06.024
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
High-throughput screening of an array of biphenylmethylamines synthesised by high-throughput solid-phase chemistry resulted in the identification of compounds with high-affinity for the 5-ht(5A) receptor. The structure-activity relationship within this series and further array synthesis led to the identification of the biphenylmethylamine derivative 11, a potent and selective 5-ht(5A) receptor antagonist. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4014 / 4018
页数：5
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