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Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists
- Authors
- Hoang Nam Vu; Kim, Ji Young; Hassan, Ahmed H. E.; Choi, Kihang; Park, Jong-Hyun; Park, Ki Duk; Lee, Jae Kyun; Pae, Ae Nim; Choo, Hyunah; Min, Sun-Joon; Cho, Yong Seo
- Issue Date
- 1-1월-2016
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Metabotropic glutamate receptor; Antagonist; Picolinamides; Thiazole-2-carboxamides; Molecular docking
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.1, pp.140 - 144
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 26
- Number
- 1
- Start Page
- 140
- End Page
- 144
- ISSN
- 0960-894X
- 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. (C) 2015 Elsevier Ltd. All rights reserved.
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