From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies

被引：58

作者：

Eildal, Jonas N. N. ^{[1
,2
]}

Andersen, Jacob ^{[1
,2
]}

Kristensen, Anders S. ^{[1
]}

Jorgensen, Anne Marie ^{[2
]}

Bang-Andersen, Benny ^{[2
]}

Jorgensen, Morten ^{[2
]}

Stromgaard, Kristian ^{[1
]}

机构：

[1] Univ Copenhagen, Fac Pharmaceut Sci, Dept Med Chem, DK-2100 Copenhagen, Denmark

[2] H Lundbeck & Co AS, Lundbeck Res Denmark, DK-2500 Copenhagen, Denmark

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 10期

关键词：

D O I：

10.1021/jm701602g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compounds were varied. The inhibitory potencies of the resulting 16 compounds were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biological activity.

引用

页码：3045 / 3048

页数：4

共 24 条

[1] Rapid, easy cyanation of aryl bromides and chlorides using nickel salts in conjunction with microwave promotion [J].