期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 1, 页码 203-208出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.134
关键词
Opioids; SAR
资金
- NATIONAL INSTITUTE ON DRUG ABUSE [K05DA000360, R01DA012180] Funding Source: NIH RePORTER
- NIDA NIH HHS [DA12180, KO5-DA00360] Funding Source: Medline
A series of 15 novel opioid derivatives were made where the prototypic phenolic-OH group of traditional opioids was replaced by a carboxamido (CONH2) group. For 2,6-methano-3-benzazocines and morphinans similar or, in a few instances, enhanced affinity for mu, delta and kappa opioid receptors was observed when the OH --> CONH2 switch was applied. For 4,5 alpha-epoxymorphinans, binding affinities for the corresponding carboxamide derivatives were much lower than the OH partner consistent with our pharmacophore hypothesis concerning carboxamide bioactive conformation. The active metabolite of tramadol and its carboxamide counterpart had comparable affinities for the three receptors. (C) 2008 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据