Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists

Publication date: 1 July 2016
Source:Bioorganic & Medicinal Chemistry, Volume 24, Issue 13
Author(s): Ting Guo, Zongjie Gan, Jie Chen, Dechuan Wang, Ling He, Qiao Song, Yungen Xu
A novel series of tetrahydroisoquinoline quaternary derivatives 4 were synthesized as peripheral κ-opioid receptor agonists. All the target compounds were evaluated in κ-opioid receptor binding assays, and compounds 4l, 4m, and 4n exhibited high affinity for κ-opioid receptor. Furthermore, compound 4l (κKi=0.94nM) produced potent antinociceptive activity in the mouse acetic acid-induced writhing assay, with lower sedative side effects than the parent compound MB-1c.

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