Remote functionalization of SCH 39166: Discovery of potent and selective benzazepine dopamine D1 receptor antagonists

被引：6

作者：

Sasikumar, T. K. ^{[1
]}

Burnett, Duane A. ^{[1
]}

Greenlee, William J. ^{[1
]}

Smith, Michelle ^{[1
]}

Fawzi, Ahmad ^{[1
]}

Zhang, Hongtao ^{[1
]}

Lachowicz, Jean E. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem & Metab Disorders, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

SCH; 39166; Ecopipam; Benzazepine; Dopamine antagonist; Obesity; D1; SCH-39166; ANALOGS; BINDING; INVIVO;

D O I：

10.1016/j.bmcl.2009.12.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel benzazepine derived dopamine D-1 antagonists have been discovered. These compounds are highly potent at D1 and showed excellent selectivity over D-2 and D-4 receptors. SAR studies revealed that a variety of functional groups are tolerated on the D-ring of known tetracyclic benzazepine analog 2, SCH 39166, leading to compounds with nanomolar potency at D-1 and good selectivity over D-2-like receptors. Published by Elsevier Ltd.

引用

页码：832 / 835

页数：4

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