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

10 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

Fingerprint

Spinal Nerves
Neuralgia
Ligation
Analgesics
Assays
Calcium
Derivatives
Therapeutics
quinoline
gabapentin

Keywords

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

ASJC Scopus subject areas

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

Cite this

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

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 5, 01.03.2013, p. 1472-1476.

Research output: Contribution to journalArticle

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. / Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain. In: Bioorganic and Medicinal Chemistry Letters. 2013 ; Vol. 23, No. 5. pp. 1472-1476.
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