8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors-Part II

被引：20

作者：

Bromidge, Steven M. ^{[1
]}

Bertani, Barbara ^{[2
]}

Borriello, Manuela ^{[2
]}

Bozzoli, Andrea ^{[2
]}

Faedo, Stefania ^{[2
]}

Gianotti, Massimo ^{[2
]}

Gordon, Laurie J. ^{[1
]}

Hill, Matthew ^{[1
]}

Zucchelli, Valeria ^{[2
]}

Watson, Jeannette M. ^{[1
]}

Zonzini, Laura ^{[2
]}

机构：

[1] GlaxoSmithKline Inc, Neurosci CEDD, Harlow CM19 5AW, Essex, England

[2] GlaxoSmithKline Inc, Neurosci CEDD, Med Res Ctr, I-37135 Verona, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 08期

关键词：

5-HT(1A/1B/1D) antagonists; Serotonin reuptake inhibitors; 5-HT(1) autoreceptors; hERG; Antidepressant; PSYCHIATRIC-DISORDERS; HERG;

D O I：

10.1016/j.bmcl.2009.02.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones have been identified as highly potent 5-HT(1A/B/D) receptor antagonists with and without additional SerT activity and a high degree of selectivity over hERG potassium channels. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2338 / 2342

页数：5

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