Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: Antagonists for the AGRP/melanocortin receptor binding

被引：37

作者：

Arasasingham, PN

Fotsch, C

Ouyang, X

Norman, MH

Kelly, MG

Stark, KL

Karbon, B

Hale, C

Baumgartner, JW

Zambrano, M

Cheetham, J

Tamayo, NA

机构：

[1] Amgen Inc, Dept Small Molecule Drug Discovery, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Dept Metab Disorders, Thousand Oaks, CA 91320 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 01期

关键词：

D O I：

10.1021/jm0255522

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action.(1) In the hypothalamus, melanocortin peptide agonists act as satiety-inducing factors that mediate their action through the melanocortin-4 receptor (MC4R) whereas AGRP is an opposing orexigenic agent. Novel inhibitors of the AGRP/MC4 binding based on (piperazinylethyl)piperazines were prepared, and their structure-activity relationship was established.

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页码：9 / 11

页数：3

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