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

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

Research output: Contribution to journalArticle

11 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1472-1476
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number5
DOIs
Publication statusPublished - 2013 Mar 1

Keywords

  • Antagonist
  • Metabotropic glutamate receptor
  • Neuropathic pain
  • Quinoline
  • Sonogashira reaction

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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