| Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors | |
Yin, Xiu-Juan1,2; Geng, Chang-An1 ; Huang, Xiao-Yan1; Chen, Hao1; Ma, Yun-Bao1; Chen, Xing-Long1,2; Sun, Chang-Li1,2; Yang, Tong-Hua1,2; Zhou, Jun1; Zhang, Xue-Mei1; Chen, Ji-Jun1
| |
| 2016 | |
| 发表期刊 | RSC ADVANCES
 |
| 卷号 | 6期号:51页码:45059-45063 |
| 摘要 | Twenty-three tropine derivatives as new melatonin receptor (MT1 and MT2) agonists were synthesized and evaluated on HEK293 cells in vitro. Derivatives 1f, 1i, 1j, 1m-1s and 1t exhibited increased agonisting activities on MT1 and MT2 receptors compared to the substrate tropine. Particularly, compound 1r showed significant agonistic activities on MT1 and MT2 receptors with EC50 values of 0.20 and 0.24 mM, respectively. The preliminary structure-activity relationships (SARs) of tropine derivatives were summarized for further investigation on melatonin receptor agonists. |
| DOI | 10.1039/c6ra06748d |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000376120100016 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/26253 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yin, Xiu-Juan,Geng, Chang-An,Huang, Xiao-Yan,et al. Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors[J]. RSC ADVANCES,2016,6(51):45059-45063. |
| APA | Yin, Xiu-Juan.,Geng, Chang-An.,Huang, Xiao-Yan.,Chen, Hao.,Ma, Yun-Bao.,...&Chen, Ji-Jun.(2016).Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors.RSC ADVANCES,6(51),45059-45063. |
| MLA | Yin, Xiu-Juan,et al."Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors".RSC ADVANCES 6.51(2016):45059-45063. |
| 条目包含的文件 | 下载所有文件 | |||||
| 文件名称/大小 | 文献类型 | 版本类型 | 开放类型 | 使用许可 | ||
| yin2016.pdf（1380KB） | 开放获取 | CC BY-NC-SA | 浏览 下载 | |||
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。
修改评论