Synthesis of 7-amino-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole derivatives displaying combined α2-adrenoceptor antagonistic and 5-HT reuptake inhibiting activities

被引：18

作者：

Andrés, JI

Alcázar, J

Alonso, JM

De Lucas, AI

Iturrino, L

Biesmans, I

Megens, AA

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, Div Janssen Cilag, Dept Med Chem, Toledo 45007, Spain

[2] Janssen Pharmaceut, Johnson & Johnson Pharmaceut Res & Dev, B-2340 Beerse, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 13期

关键词：

isoxazolines; 5-HT reuptake inhibitors; alpha(2)-antagonists; antidepressants;

D O I：

10.1016/j.bmc.2006.02.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Following a program searching for dual 5-HT reuptake inhibitors and alpha(2)-adrenoceptor antagonists started at Johnson & Johnson Pharmaceutical Research & Development, we now report on the synthesis of a series of 7-amino-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole derivatives, some of which proved to be the most potent alpha(2)-adrenoceptor blockers within this chemical class of tricyclic isoxazolines, while keeping potent 5-HT reuptake inhibiting activity. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4361 / 4372

页数：12