Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW
J Med Chem. 2019 62 (1): 378-384

PMID: 30350962 · DOI:10.1021/acs.jmedchem.8b01266

MeSH Terms (15)

Allosteric Regulation Amides Animals Central Nervous System Drug Evaluation, Preclinical Half-Life Humans Inhibitory Concentration 50 Protein Isoforms Pyrazoles Pyridines Pyrimidines Rats Receptors, Metabotropic Glutamate Structure-Activity Relationship

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