5-Cyclic Amine-3-arylsulfonylindazoles as Novel 5-HT6 Receptor Antagonists

被引：20

作者：

Haydar, Simon N. ^{[1
]}

Yun, Heedong ^{[1
]}

Andrae, Patrick M. ^{[1
]}

Mattes, James ^{[1
]}

Zhang, Jean ^{[2
]}

Kramer, Angela ^{[2
]}

Smith, Deborah L. ^{[2
]}

Huselton, Christine ^{[3
]}

Graf, Radka ^{[2
]}

Aschmies, Suzan ^{[2
]}

Schechter, Lee E. ^{[2
]}

Comery, Thomas A. ^{[2
]}

Robichaud, Albert J. ^{[1
]}

机构：

[1] Wyeth Ayerst Res, Chem Sci, Princeton, NJ 08543 USA

[2] Wyeth Ayerst Res, Discovery Neurosci, Princeton, NJ 08543 USA

[3] Wyeth Ayerst Res, Drug Safety & Metab, Collegeville, PA 19426 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 06期

关键词：

ACETYLCHOLINE-RELEASE; POTENT; DERIVATIVES; LOCALIZATION; DISCOVERY; SB-271046; HYDROGEN; LIGANDS; CORTEX;

D O I：

10.1021/jm901674f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 5-cyclic amine-3-arylsulfonylindazoles were prepared, and several analogues within this class have been identified as high-affinity 5-HT6 receptor ligands with improved pharmacokinetic and pharmacological properties. One selected example, 18b, showed good brain penetrability and a generally favorable pharmacokinetic profile with procognitive efficacy in the rat novel object recognition assay. The synthesis and structure activity relationship of this potent class are discussed.

引用

页码：2521 / 2527

页数：7

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