Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors

doi:10.1039/c6ra06748d

	Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors
	Yin, Xiu-Juan 1,2; Geng, Chang-An1 ; Huang, Xiao-Yan 1; Chen, Hao 1; Ma, Yun-Bao 1; Chen, Xing-Long 1,2; Sun, Chang-Li 1,2; Yang, Tong-Hua 1,2; 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.

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