Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain

We described here the synthesis and biological evaluation of mGluR5 antagonists containing a quinoline ring structure. Using intracellular calcium mobilization assay (FDSS assay), we identified compound 5n, showing high inhibitory activity against mGluR5. In addition, it was found that compound 5n h...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-03, Vol.23 (5), p.1472-1476
Main Authors: Son, Myung-Hee, Kim, Ji Young, Lim, Eun Jeong, Baek, Du-Jong, Choi, Kihang, Lee, Jae Kyun, Pae, Ae Nim, Min, Sun-Joon, Cho, Yong Seo
Format: Article
Language:English
Subjects:
Acetylene - analogs & derivatives
Acetylene - chemistry
Acetylene - pharmacology
analgesics
Antagonist
antagonists
calcium
chemistry
HEK293 Cells
Humans
Metabotropic glutamate receptor
nerve tissue
Neuralgia - drug therapy
Neuropathic pain
pain
Quinoline
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacology
Receptor, Metabotropic Glutamate 5 - antagonists & inhibitors
Sonogashira reaction
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Summary:We described here the synthesis and biological evaluation of mGluR5 antagonists containing a quinoline ring structure. Using intracellular calcium mobilization assay (FDSS assay), we identified compound 5n, showing high inhibitory activity against mGluR5. In addition, it was found that compound 5n has excellent stability profile. Finally, this compound exhibited favorable analgesic effects in spinal nerve ligation model of neuropathic pain, which is comparable to gabapentin.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.12.056