Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists

Hoang Nam Vu, Ji Young Kim, Ahmed H E Hassan, Kihang Choi, Jong Hyun Park, Ki Duk Park, Jae Kyun Lee, Ae Nim Pae, Hyunah Choo, Sun Joon Min, Yong Seo Cho

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

We described here the synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as potential mGluR5 antagonists. We found that a series of thiazole derivatives 6 showed better inhibitory activity against mGluR5. Compounds 6bc and 6bj have been identified as potent antagonists (IC50 = 274 and 159 nM) showing excellent in vitro stability profile. Molecular docking study using the crystal structure of mGluR5 revealed that our compounds 6bc and 6bj fit the allosteric binding site of mavoglurant well.

Original languageEnglish
Pages (from-to)140-144
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number1
DOIs
Publication statusPublished - 2016 Jan 1

Keywords

  • Antagonist
  • Metabotropic glutamate receptor
  • Molecular docking
  • Picolinamides
  • Thiazole-2-carboxamides

ASJC Scopus subject areas

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

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