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

Title
Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists
Authors
부 호앙 남김지영Ahmed Helmy Ebraheem Hassan최기항박종현박기덕이재균배애님추현아민선준조용서
Keywords
metabotropic glutamate receptor; antagonist; picolinamides; thiazole-2- carboxamides; molecular docking
Issue Date
2015-11
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 게재예정, 게재예정
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.
URI
http://pubs.kist.re.kr/handle/201004/50951
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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