Aryl piperazine melanocortin MC4 receptor agonists

被引：50

作者：

Dyck, B

Parker, J

Phillips, T

Carter, L

Murphy, B

Summers, R

Hermann, J

Baker, T

Cismowski, M

Saunders, J

Goodfellow, V

机构：

[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92121 USA

[2] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92121 USA

[3] Neurocrine Biosci Inc, Dept Mol Biol, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(03)00796-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC50 = 24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or other melancortin receptors. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3793 / 3796

页数：4

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