Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands

被引：56

作者：

Descamps-François, C

Yous, S

Chavatte, P

Audinot, V

Bonnaud, A

Boutin, JA

Delagrange, P

Bennejean, C

Renard, P

Lesieur, D

机构：

[1] Univ Lille 2, Fac Pharm, Chim Therapeut Lab, F-59006 Lille, France

[2] Inst Rech Int Serv, Courbevoie, France

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 07期

关键词：

D O I：

10.1021/jm0255872

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis and binding properties at MT1 and MT2 receptors of the first example of agomelatine (N-[2-(7-methoxynaphth-1-yl)ethyl] acetamide) dimers in which two agomelatine moieties are linked together through their methoxy substituent by a polymethylene side chain according to the "bivalent ligand" approach. Some of these compounds behave as MT1-selective ligands. The most selective one (5) behaves as an antagonist.

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页码：1127 / 1129

页数：3

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