Synthesis and biological activities of N-indolalkyl piperidine derivatives and their analogues
文献类型：期刊论文
| 作者 | WANG Guan2; ZHANG Gui-sen3; GUO Lin3; YU Lei-ping1; LI Jian-qi2 |
| 刊名 | Chinese Journal of Medicinal Chemistry
 |
| 出版日期 | 2009 |
| 卷号 | 19期号:3页码:161-169 |
| 关键词 | N-indolalkyl piperidine derivatives synthesis 5-HT reuptake inhibitors 5-HT_(2A) recepetor non-opioid analgesic activity |
| ISSN号 | 1005-0108 |
| 其他题名 | N-吲哚烷基哌啶类化合物及其类似物的合成和活性研究 |
| 文献子类 | Article |
| 英文摘要 | Aim According to the targets of 5-HT transporter and 5-HT_(2A) receptor, a series of N-indolalkyl piperidine derivatives and their analogues were synthesized and tested for their biological activities. Methods Eighteen compounds were prepared from benzo-fused nitrogen heterocycles through N-alkylation and then condensation with derivatives of piperidine or piperazine. All of them were carried out in vitro pharmacological test for the 5-HT transporter and 5-HT_(2A)receptor. Among the tested compounds 10c and 10e were trialed analgesic activities in both mice writhing and mice hot plate models. Results and conclusion Eighteen novel compounds were prepared; and their structures were confirmed by ~1H-NMR and HRMS. Most of them showed high affinity for the 5-HT transporter and 5-HT_(2A)receptor.10c and 10e exhibited potent analgesic activities in two models in vivo with low affinity to mu, delta, kappa receptors, which is a chance to find a better precursor of non-opioid analgesic for further optimization. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:3543123 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/267989]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.Shanghai Institute of Materia,Chinese Academy of Sciences, Shanghai 201203, China. 2.Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.; 3.Jiangsu NHWA Pharmaceutical Co.,Ltd., Xuzhou, Jiangsu 221007, China.; |
| 推荐引用方式 GB/T 7714 | WANG Guan,ZHANG Gui-sen,GUO Lin,et al. Synthesis and biological activities of N-indolalkyl piperidine derivatives and their analogues[J]. Chinese Journal of Medicinal Chemistry,2009,19(3):161-169. |
| APA | WANG Guan,ZHANG Gui-sen,GUO Lin,YU Lei-ping,&LI Jian-qi.(2009).Synthesis and biological activities of N-indolalkyl piperidine derivatives and their analogues.Chinese Journal of Medicinal Chemistry,19(3),161-169. |
| MLA | WANG Guan,et al."Synthesis and biological activities of N-indolalkyl piperidine derivatives and their analogues".Chinese Journal of Medicinal Chemistry 19.3(2009):161-169. |
入库方式： OAI收割
来源：上海药物研究所
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