SB-656104-A:: A novel 5-HT7 receptor antagonist with improved in vivo properties

被引：67

作者：

Forbes, IT ^{[1
]}

Douglas, S ^{[1
]}

Gribble, AD ^{[1
]}

Ife, RJ ^{[1
]}

Lightfoot, AP ^{[1
]}

Garner, AE ^{[1
]}

Riley, GJ ^{[1
]}

Jeffrey, P ^{[1
]}

Stevens, AJ ^{[1
]}

Stean, TO ^{[1
]}

Thomas, DR ^{[1
]}

机构：

[1] GlaxoSmithKline, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(02)00690-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A focused SAR study around the previously reported selective 5-HT7 receptor antagonist, SB-269970-A has resulted in the identification of a structurally related analogue having an improved pharmacokinetic profile. Replacement of the phenolic group in SB-269970-A with an indole moiety, and replacement of the piperidinyl 4-methyl group with a heterocyclic ring system proved to be the key changes leading to the identification of SB-656104-A. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3341 / 3344

页数：4

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