Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]-oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists

被引：21

作者：

Coats, SJ ^{[1
]}

Schulz, MJ ^{[1
]}

Carson, JR ^{[1
]}

Codd, EE ^{[1
]}

Hlasta, DJ ^{[1
]}

Pitis, PM ^{[1
]}

Stone, DJ ^{[1
]}

Zhang, SP ^{[1
]}

Colburn, RW ^{[1
]}

Dax, SL ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Durg Discovery, Spring House, PA 19477 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 22期

关键词：

opioid; delta; mu; parallel; antinociception;

D O I：

10.1016/j.bmcl.2004.09.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two parallel synthetic methods were developed to explore the structure-activity relationships (SAR) of a series of potent opioid agonists. This series of tropanylidene benzamides proved extremely tolerant of structural variation while maintaining excellent opioid activity. Evaluation of several representative compounds from this series in the mouse hot plate test revealed potent antinociceptive effects upon oral administration. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5493 / 5498

页数：6

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