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

Abstract

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.

• Authors: Myung-Hee Son, Ji Young Kim, Eun Jeong Lim, Du-Jong Baek, Kihang Choi, Jae Kyun Lee, Ae Nim Pae, Sun-Joon Min, Yong Seo Cho
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 5 Pg. 1472-6 (Mar 01 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 23333207 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Ltd. All rights reserved.

Chemical References

• Quinolines
• Receptor, Metabotropic Glutamate 5
• Acetylene

Topics

• Acetylene (analogs & derivatives, chemistry, pharmacology)
• HEK293 Cells
• Humans
• Neuralgia (drug therapy)
• Quinolines (chemical synthesis, chemistry, pharmacology)
• Receptor, Metabotropic Glutamate 5 (antagonists & inhibitors)