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.
DOI10.1039/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
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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.
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