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
收藏
页码：3341 / 3344
页数：4
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