Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5-a]pyrimidine-5-carboxamide and Thieno[3,2-b]pyridine-5-carboxamide Cores was written by Childress, Elizabeth S.;Wieting, Joshua M.;Felts, Andrew S.;Breiner, Megan M.;Long, Madeline F.;Luscombe, Vincent B.;Rodriguez, Alice L.;Cho, Hyekyung P.;Blobaum, Anna L.;Niswender, Colleen M.;Emmitte, Kyle A.;Conn, P. Jeffrey;Lindsley, Craig W.. And the article was included in Journal of Medicinal Chemistry in 2019.HPLC of Formula: 51834-97-0 This article mentions the following:
A scaffold hopping exercise from a monocyclic mGlu2 NAM with poor rodent PK led to two novel heterobicyclic series of mGlu2 NAMs based on either a functionalized pyrazolo[1,5-a]pyrimidine-5-carboxamide core or a thieno[3,2-b]pyridine-5-carboxamide core. These novel analogs possess enhanced rodent PK, while also maintaining good mGlu2 NAM potency, selectivity (vs. mGlu3 and the remaining six mGlu receptors), and high CNS penetration. Interestingly, SAR was divergent between the new 5,6-heterobicyclic systems. In the experiment, the researchers used many compounds, for example, 5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0HPLC of Formula: 51834-97-0).
5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. HPLC of Formula: 51834-97-0