Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-thiocarboxamido and 8-thioformamido derivatives of cyclazoeine

被引：15

作者：

Wentland, MP ^{[1
]}

Sun, XF

Bu, YG

Lou, RL

Cohen, DJ

Bidlack, JM

机构：

[1] Rensselaer Polytech Inst, Dept Chem & Chem Biol, Troy, NY 12180 USA

[2] Univ Rochester, Sch Med & Dent, Dept Pharmacol & Physiol, Rochester, NY 14642 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 10期

关键词：

opiate SAR;

D O I：

10.1016/j.bmcl.2005.03.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

8 -Position variants of cyclazocine have been made where the phenolic 8-OH was replaced by thioamide, amidine, guanidine, urea and thiourea groups. High affinity for opioid receptors was observed for the 8-CSNH2 and 8-NHCHS analogues indicating that these groups are isosteric with not only the 8-OH but with the previously synthesized 8-CONH2 and 8-NHCHO cyclazocine derivatives. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2547 / 2551

页数：5

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