Vu, Hoang Nam published the artcileSynthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists, Product Details of C6H7ClN2, the main research area is thiazolecarboxamide aryl preparation metabotropic glutamate receptor antagonist; picolinamide aryl preparation metabotropic glutamate receptor antagonist; Antagonist; Metabotropic glutamate receptor; Molecular docking; Picolinamides; Thiazole-2-carboxamides.
Herein the synthesis and biol. evaluation of picolinamides and thiazole-2-carboxamides as potential mGluR5 antagonists are described. It was found that a series of N-aryl-4-R-2-thiazolecarboxamides (R = Br, Me, CN; aryl = 3-FC6H4, 3-NCC6H4, 2-pyridyl, 6-chloro-2-pyridyl, etc.) (I) showed better inhibitory activity against mGluR5. The compounds I (R = Br; aryl = 3-BrC6H4, 6-methyl-2-pyridyl) have been identified as potent antagonists (IC50 = 274 and 159 nM) showing excellent in vitro stability profile. Mol. docking study using the crystal structure of mGluR5 revealed that these two compounds fit the allosteric binding site of mavoglurant well.
Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Product Details of C6H7ClN2.