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[褪黑素能受体的新型萘基配体]

[New naphthalenic ligands of melatoninergic receptors].

作者信息

Adam G, Guardiola-Lemaitre B, Yous S, Lesieur D, Morgan P, Howell H E, Andrieux J, Caignard D H, Pfeiffer B, Renard P

机构信息

IRIS-SERVIER, Courbevoie, France.

出版信息

J Pharm Belg. 1992 Jul-Aug;47(4):374-80.

PMID:1328595
Abstract

Twenty three naphthalenic bio-isosteres of melatonin have been synthesized. The main structural variations concerned the acylamino substituents of the side chain and the alkoxy group on the 7-position of the naphthalene. Some of these compounds show greater affinity than melatonin itself for the melatonin receptor. The results of this study provide new informations on the structure affinity relationships and on the mode of interaction at the melatonin binding site.

摘要

已合成了23种褪黑素的萘生物电子等排体。主要的结构变化涉及侧链的酰氨基取代基和萘7位上的烷氧基。其中一些化合物对褪黑素受体的亲和力比褪黑素本身更强。这项研究的结果提供了关于结构亲和力关系以及褪黑素结合位点相互作用模式的新信息。

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