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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
- Author
- 민선준
- Keywords
- Metabotropic glutamate receptor; Antagonist; Picolinamides; Thiazole-2-carboxamides; Molecular docking; NEGATIVE ALLOSTERIC MODULATORS; GASTROESOPHAGEAL-REFLUX DISEASE; FRAGILE-X-SYNDROME; NEUROPATHIC PAIN; PHARMACOLOGY; MGLU(5); RATS; IDENTIFICATION; SYMPTOMS; EXPOSURE
- Issue Date
- 2016-01
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 26, No. 1, Page. 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.
- URI
- https://www.sciencedirect.com/science/article/pii/S0960894X15302213http://hdl.handle.net/20.500.11754/48924
- ISSN
- 0960-894X; 1464-3405
- Appears in Collections:
- COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > ETC
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