Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)
文献类型：期刊论文
| 作者 | Zheng, JB; Wen, R; Luo, XM ; Lin, GQ; Zhang, JG; Xu, LF; Guo, LH; Jiang, HL
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2006 |
| 卷号 | 16期号:1页码:225-227 |
| 关键词 | GABA uptake inhibitors GAT1 antiepileptic N-diaryl-alkenyl-piperidinecarboxylic acid derivatives |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2005.09.004 |
| 文献子类 | Article |
| 英文摘要 | Twenty novel N-diarylalkenyl-piperidinecarboxylic acid derivatives were synthesized and evaluated as gamma-aminobutyric acid uptake inhibitors. The biological assay showed that (R)-1-[4,4-bis(3-phenoxymethyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic hydrochloride (4e) possessed almost as strong GAT1 inhibitory activity as tiagabine. The synthesis and structure-activity relationships are discussed. (c) 2005 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MOUSE-BRAIN ; RAT-BRAIN ; TRANSPORTER ; TIAGABINE ; EPILEPSY ; EXPRESSION ; DISEASE |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000233516200048 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273697]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Wen, R |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China 2.Fudan Univ, Dept Med Chem, Shanghai 200032, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, Shanghai 200032, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zheng, JB,Wen, R,Luo, XM,et al. Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2006,16(1):225-227. |
| APA | Zheng, JB.,Wen, R.,Luo, XM.,Lin, GQ.,Zhang, JG.,...&Jiang, HL.(2006).Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,16(1),225-227. |
| MLA | Zheng, JB,et al."Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 16.1(2006):225-227. |
入库方式： OAI收割
来源：上海药物研究所
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