2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles:: New templates for 5-HT2C agonists

被引：26

作者：

Ennis, MD ^{[1
]}

Hoffman, RL

Ghazal, NB

Olson, RM

Knauer, CS

Chio, CL

Hyslop, DK

Campbell, JE

Fitzgerald, LW

Nichols, NF

Svensson, KA

McCall, RB

Haber, CL

Kagey, ML

Dinh, DM

机构：

[1] Pharmacia Corp, Med Chem 3, Kalamazoo, MI 49009 USA

[2] Pharmacia Corp, CNS Dis, Kalamazoo, MI 49009 USA

[3] Pharmacia Corp, Discovery Technol, Kalamazoo, MI 49009 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(03)00403-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and synthesis of the novel 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indole 5 is described. This azepinoindole has excellent affinity for 5-HT2C (K-i 4.8 nM) and modest selectivity over 5-HT2A (similar to4-fold). Several N- and C-11-substituted analogues of 5 were prepared, as were a number of biaryl indoline derivatives. The anxiolytic potential for the azepinoindole template 5 is demonstrated by activity in a mouse shock-aggression assay. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：2369 / 2372

页数：4

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