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

页码：67 / 74

页数：8

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