trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines:: A novel class of μ-selective opioid antagonists

被引：22

作者：

Le Bourdonnec, B

Belanger, S

Cassel, JA

Stabley, GJ

DeHaven, RN

Dolle, RE

机构：

[1] Adolor Corp, Dept Chem, Exton, PA 19341 USA

[2] Adolor Corp, Dept Pharmacol, Exton, PA 19341 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 24期

关键词：

D O I：

10.1016/j.bmcl.2003.09.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of p opioid receptor antagonists. The CONH, group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine nitrogen position led to the identification of several ligands displaying high affinity toward the cloned human P opioid receptors, good selectivity mu/delta, mu/kappa, and potent in vitro antagonist activity. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：4459 / 4462

页数：4

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