3-pyrroline containing arylacetamides: A novel series of remarkably selective kappa-agonists
文献类型：期刊论文
| 作者 | Mou, QY; Chen, J ; Zhu, YC; Zhou, DH; Chi, ZQ; Long, YQ
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2002-09-02 |
| 卷号 | 12期号:17页码:2287-2290 |
| ISSN号 | 0960-894X |
| DOI | 10.1016/S0960-894X(02)00429-8 |
| 文献子类 | Article |
| 英文摘要 | A series of 2-(substituted phenyl)-N-methyl-N-[(1S)-1-(substituted alkyl)-2-(1-(3-pyrrolinyl))ethyl]acetamides were synthesized and evaluated as highly selective kappa-agonists with K-i values in low nanomolar range. 3-Pyrroline incorporated into the basic amino functionality in combination with 2-(methylthio)ethyl substituent on the carbon adjacent to the amide nitrogen remarkably enhanced the K-selectivity. 3,4-Dichlorophenyl derivative le was found the most potent and selective analgesic in this series with ED50 value of 0.023 mg/kg. (C) 2002 Elsevier Science Ltd. All rights reserved. |
| WOS关键词 | OPIOID RECEPTOR AGONISTS ; OHMEFENTANYL ; EXPRESSION ; POTENT |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000177603200006 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274331]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Long, YQ |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Mou, QY,Chen, J,Zhu, YC,et al. 3-pyrroline containing arylacetamides: A novel series of remarkably selective kappa-agonists[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2002,12(17):2287-2290. |
| APA | Mou, QY,Chen, J,Zhu, YC,Zhou, DH,Chi, ZQ,&Long, YQ.(2002).3-pyrroline containing arylacetamides: A novel series of remarkably selective kappa-agonists.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,12(17),2287-2290. |
| MLA | Mou, QY,et al."3-pyrroline containing arylacetamides: A novel series of remarkably selective kappa-agonists".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 12.17(2002):2287-2290. |
入库方式： OAI收割
来源：上海药物研究所
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