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

Twenty-three tropine derivatives as new melatonin receptor (MT 1 and MT 2 ) agonists were synthesized and evaluated on HEK293 cells in vitro . Derivatives 1f , 1i , 1j , 1m-1s and 1t exhibited increased agonisting activities on MT 1 and MT 2 receptors compared to the substrate tropine. Particularly,...

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Bibliographic Details
Published in:RSC advances 2016-01, Vol.6 (51), p.4559-4563
Main Authors: Yin, Xiu-Juan, Geng, Chang-An, Huang, Xiao-Yan, Chen, Hao, Ma, Yun-Bao, Chen, Xing-Long, Sun, Chang-Li, Yang, Tong-Hua, Zhou, Jun, Zhang, Xue-Mei, Chen, Ji-Jun
Format: Article
Language:English
Subjects:
Biocompatibility
Biomedical materials
Derivatives
Melatonin
Receptors
SARS
Surgical implants
Synthesis
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Summary:Twenty-three tropine derivatives as new melatonin receptor (MT 1 and MT 2 ) agonists were synthesized and evaluated on HEK293 cells in vitro . Derivatives 1f , 1i , 1j , 1m-1s and 1t exhibited increased agonisting activities on MT 1 and MT 2 receptors compared to the substrate tropine. Particularly, compound 1r showed significant agonistic activities on MT 1 and MT 2 receptors with EC 50 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. Twenty-three tropine derivatives as new melatonin receptor (MT 1 and MT 2 ) agonists were synthesized and evaluated on HEK293 cells in vitro .
ISSN:2046-2069
2046-2069
DOI:10.1039/c6ra06748d