SB-656104-A:: A novel 5-HT7 receptor antagonist with improved in vivo properties
SB-656104-A:: A novel 5-HT7 receptor antagonist with improved in vivo properties
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DOI：
10.1016/s0960-894x(02)00690-x
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发表时间：
2002-11-18
影响因子：
2.7
通讯作者：
Thomas, DR
中科院分区：
文献类型：
--
作者：
Forbes, IT;Douglas, S;Thomas, DR
一项针对先前报道的选择性5-HT7受体拮抗剂SB-269970-A的重点SAR研究已经确定了一种结构相关的类似物，具有改善的药代动力学特征。将SB-269970-A中的酚基替换为吲哚基团，并将胡椒酰4-甲基替换为杂环体系是鉴定SB-656104-A的关键变化。(C) 2002 Elsevier Science Ltd.版权所有。
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.