[6,7]-Heterocycle-Fused 14-Hydroxymorphinan Derivatives: Design, Synthesis, and Opioid Receptor Activity
文献类型：期刊论文
| 作者 | Li, Fuying2; Yin, Chenlei1; Chen, Jie3; Liu, Jinggen3 ; Xie, Xin1; Zhang, Ao2
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| 刊名 | CHEMMEDCHEM
 |
| 出版日期 | 2009-12 |
| 卷号 | 4期号:12页码:2103-2110 |
| 关键词 | 14-hydroxymorphinans aminothiazoles drug abuse imidazo[2,1-b]thiazoles opioid receptors |
| ISSN号 | 1860-7179 |
| DOI | 10.1002/cmdc.200900308 |
| 文献子类 | Article |
| 英文摘要 | A series of new 14-hydroxymorphinan analogues with a thiazole or imidazo[2,1-b]thiazole fragment as the heterocyclic function fused to ring C were designed and synthesized. These compounds can be viewed as the result of a direct modification at ring C of the 14-hydroxymorphinan scaffold. Among these compounds, three were identified as having potent binding affinity (similar to 1 nm) at both kappa and mu receptors, and acting as agonists at kappa and partial agonists or antagonists at kappa, receptors. In view of the promising results from studies on compounds with mixed kappa and mu. receptor activities, these new compounds warrant further investigation. |
| WOS关键词 | KAPPA-AGONIST ; BIOLOGICAL EVALUATION ; LIGANDS ; ANTAGONISTS ; OXYMORPHONE ; NALTRINDOLE ; NALTREXONE ; INHIBITORS ; AFFINITY ; ANALOGS |
| 资助项目 | Chinese Academy of Sciences[00000000] ; Chinese National Science Foundation[30772625] ; Shanghai Commission of Science and Technology[07pj14104] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000272739800016 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279072]  |
| 专题 | 药理学第二研究室 药物化学研究室 国家新药筛选中心 |
| 通讯作者 | Liu, Jinggen |
| 作者单位 | 1.Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 2.Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, Shanghai 201203, Peoples R China; 3.Shanghai Inst Mat Med, Neuropharmacol Lab, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Li, Fuying,Yin, Chenlei,Chen, Jie,et al. [6,7]-Heterocycle-Fused 14-Hydroxymorphinan Derivatives: Design, Synthesis, and Opioid Receptor Activity[J]. CHEMMEDCHEM,2009,4(12):2103-2110. |
| APA | Li, Fuying,Yin, Chenlei,Chen, Jie,Liu, Jinggen,Xie, Xin,&Zhang, Ao.(2009).[6,7]-Heterocycle-Fused 14-Hydroxymorphinan Derivatives: Design, Synthesis, and Opioid Receptor Activity.CHEMMEDCHEM,4(12),2103-2110. |
| MLA | Li, Fuying,et al."[6,7]-Heterocycle-Fused 14-Hydroxymorphinan Derivatives: Design, Synthesis, and Opioid Receptor Activity".CHEMMEDCHEM 4.12(2009):2103-2110. |
入库方式： OAI收割
来源：上海药物研究所
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