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
收藏
页码：832 / 835
页数：4
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