Synthesis and evaluation of novel-N-2-(bis-arylmethoxy)ethyl-N'-aralkyl-alpha,omega-alkanediamines as potent and selective dopamine reuptake inhibitors: Seco analogs of GBR12935 and GBR12909

被引：8

作者：

Hanson, RN ^{[1
]}

Choi, SW ^{[1
]}

Elmaleh, DR ^{[1
]}

Fischman, AJ ^{[1
]}

机构：

[1] MASSACHUSETTS GEN HOSP,DIV NUCL MED,DEPT RADIOPHARMACEUT CHEM,BOSTON,MA 02114

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(97)10053-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of analogs of the N-L[2-bis arylmethoxy]-N'-phenylpropyl-piperazines GBR12909 and 12935 was synthesized and evaluated as inhibitors of synaptic monoamine transporters. The data indicated that all of the new compounds demonstrated a selectivity for the dopamine transporter compared to the other monoamine transporters with IC50 values approaching 10 nM. The results suggest that the internal piperazine moiety is not required for activity and may be replaced with a more flexible diamine unit. (C) 1997 Elsevier Science Ltd.

引用

页码：2559 / 2564

页数：6

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