Synthesis and μ-opioid receptor affinity of a new series of nitro substituted 3,8-diazabicyclo[3.2.1]octane derivatives

被引：7

作者：

Barlocco, D

Cignarella, G

Vianello, P

Villa, S

Pinna, GA

Fadda, P

Fratta, W

机构：

[1] Ist Chim Farmaceut & Tossicol, I-20131 Milan, Italy

[2] Ist Chim Farmaceut, I-07100 Sassari, Italy

[3] Dipartimento Neurosci, I-09100 Cagliari, Italy

来源：

FARMACO | 1998年 / 53卷 / 8-9期

关键词：

opioid receptors; analgesic activity; diazabicyclooctane;

D O I：

10.1016/S0014-827X(98)00065-2

中图分类号：

R9 [药学];

学科分类号：

1007 [药学];

摘要：

A new series of analogues (1c-j; 2c-i) of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (1a,b; 2a,b) was synthesized and tested for their affinity towards mu-opioid receptors. Modifications were introduced either at the cinnamyl or the acyl side chains. The majority of the new compounds, with the exception of 1c,j and 2c, showed K-i values better or comparable with those of the models. (C) 1998 Elsevier Science S.A. All rights reserved.

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收藏

页码：557 / 562

页数：6

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