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

被引：6

作者：

Yin, Xiu-Juan ^{[1
,2
]}

Geng, Chang-An ^{[1
]}

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, Jun ^{[1
]}

Zhang, Xue-Mei ^{[1
]}

Chen, Ji-Jun ^{[1
]}

机构：

[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

来源：

RSC ADVANCES | 2016年 / 6卷 / 51期

基金：

中国国家自然科学基金;

关键词：

COCAINE; BINDING; BENZTROPINE;

D O I：

10.1039/c6ra06748d

中图分类号：

O6 [化学];

学科分类号：

0703 ;

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.

引用

页码：45059 / 45063

页数：5

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