Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368804 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,