Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists

被引：14

作者：

Jeanty, Matthieu ^{[1
]}

Suzenet, Franck ^{[1
]}

Delagrange, Philippe ^{[2
]}

Nosjean, Olivier ^{[2
]}

Boutin, Jean A. ^{[2
]}

Caignard, Daniel H. ^{[2
]}

Guillaumet, Gerald ^{[1
]}

机构：

[1] Univ Orleans, CNRS, UMR 6005, ICOA, F-45067 Orleans 2, France

[2] Inst Rech Servier, Dept Sci Expt, F-92150 Suresnes, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 08期

关键词：

Melatonin; 7-Azaindole; MT receptors agonists; RECEPTOR ANTAGONISTS; QUINONE REDUCTASE-2; MT2; RECEPTORS; BINDING-SITE; LIGANDS; AGOMELATINE; MAMMALS; ANALOGS; ENZYME;

D O I：

10.1016/j.bmcl.2011.02.097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 7-azaindolic ligands bearing a methoxy group and a N-acetyl chain as melatoninergic pharmacophores were synthesized and their binding affinities towards MT1 and MT2 receptors were evaluated. Compounds 7a-c and 12 (cyclohexyl ring connected at C-2 and C-3 position) appears as important melatonin MT2 and MT1 receptors agonists. On the other hand, the presence of basic groups (amines) at position C-3 was detrimental to the melatoninergic affinities. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2316 / 2319

页数：4

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