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 |
| 通讯作者 | Wen, R (reprint author), Fudan Univ, Dept Med Chem, Shanghai 200032, Peoples R China.,rwen@shmu.edu.cn |
| 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. |
| 学科主题 | Pharmacology & Pharmacy; Chemistry |
| 类目[WOS] | Chemistry, Medicinal ; Chemistry, Organic |
| 关键词[WOS] | MOUSE-BRAIN ; RAT-BRAIN ; TRANSPORTER ; TIAGABINE ; EPILEPSY ; EXPRESSION ; DISEASE |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000233516200048 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1651]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 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. |
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