Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists
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.
Vu, Hoang Nam,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
Synthesis of pyridinecarbothionylaminopyridines and conversion of thioamide to amide
Pyridinecarbothionylaminopyridines as structural isomers were obtained by the reactions of 2,3-and 2-4-lutidine with aminopyridines and sulfur. Reaction of 2,6-lutidine with active methyl group anilines in the presence of sulfur gave the desired thioamides 5. Reaction of synthesized thioamides 5 with sulfur and SiO2 or SeO2 gave the corresponding amide 6. We now report conversion of thioamide to amide by using oxidizing inorganic reagent.
Choi,Yoon,Lee,Kim,Kim,Jung,Hahn
experimental part
p. 4987 - 4989
(2012/07/13)
Pyridine-2-carboxyamide derivatives
The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.
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Page/Page column 17
(2008/06/13)
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