Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists

被引：0
|
作者：
Tran, Joe A. [1 ]
Arellano, Melissa [1 ]
Fleck, Beth A. [2 ]
Pontillo, Joseph [1 ]
Marinkovic, Dragan [1 ]
Tucci, Fabio C. [1 ,3 ]
Wen, Jenny [3 ]
Saunders, John [1 ]
Chen, Chen [1 ]
机构：
[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92130 USA
[2] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92130 USA
[3] Neurocrine Biosci Inc, Dept Preclin Dev, San Diego, CA 92130 USA
来源：
MEDICINAL CHEMISTRY | 2008年 / 4卷 / 01期
关键词：
melanocortin-4; receptor; antagonist; piperazinephenethylamine; synthesis;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of piperazinephenethylamines were synthesized to study the contribution of a basic amine to binding affinity at the melanocortin-4 receptor. Several potent compounds from this series possessed subnanomolar K-i values in a competition binding assay.
引用
收藏
页码：67 / 74
页数：8
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