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

被引：40

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

页码：4014 / 4018

页数：5

共 10 条

[1] Ligand identification for G-protein-coupled receptors: a lead generation perspective [J].