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	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
刊名	RSC ADVANCES
	2016
卷号	6期号:51页码:45059-45063
英文摘要	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.
类目[WOS]	Chemistry, Multidisciplinary
研究领域[WOS]	Chemistry
关键词[WOS]	BINDING ; COCAINE ; BENZTROPINE ; ANTAGONISTS ; DISCOVERY
收录类别	SCI
语种	英语
WOS记录号	WOS:000376120100016
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/26253]
专题	昆明植物研究所_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.

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