Propionylpiperazines as human melanocortin-4 receptor ligands

被引：12

作者：

Chen, Caroline W.

Tran, Joe A.

Jiang, Wanlong

Tucci, Fabio C.

Arellano, Melissa

Wen, Jenny

Fleck, Beth A.

Marinkovic, Dragan

White, Nicole S.

Pontillo, Joseph

Saunders, John

Madan, Ajay

Foster, Alan C.

Chen, Chen

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 Neurosci, San Diego, CA 92130 USA

[4] Neurocrine Biosci Inc, Dept Preclin Dev, San Diego, CA 92130 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 18期

关键词：

propionylpiperazine; melanocortin-4; receptor; antagonist; pharmacokinetic;

D O I：

10.1016/j.bmcl.2006.06.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice. (c) 2006 Elsevier Ltd. All rights reserved.

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页码：4800 / 4803

页数：4

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