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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
2016-01-01
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.26, no.1, pp.140 - 144
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.
Keywords
NEGATIVE ALLOSTERIC MODULATORS; GASTROESOPHAGEAL-REFLUX DISEASE; FRAGILE-X-SYNDROME; NEUROPATHIC PAIN; PHARMACOLOGY; MGLU(5); RATS; IDENTIFICATION; SYMPTOMS; EXPOSURE; NEGATIVE ALLOSTERIC MODULATORS; GASTROESOPHAGEAL-REFLUX DISEASE; FRAGILE-X-SYNDROME; NEUROPATHIC PAIN; PHARMACOLOGY; MGLU(5); RATS; IDENTIFICATION; SYMPTOMS; EXPOSURE; Metabotropic glutamate receptor; Antagonist; Picolinamides; Thiazole-2-carboxamides; Molecular docking
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/124521
DOI
10.1016/j.bmcl.2015.11.012
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KIST Article > 2016
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