Discovery, Synthesis, and Structure-Activity Relationship Development of a Series of N-(4-Acetamido)phenylpicolinamides as Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 (mGlu(4)) with CNS Exposure in Rats

作者：Engers Darren W; Field Julie R; Le Uyen; Zhou Ya; Bolinger Julie D; Zamorano Rocio; Blobaum Anna L; Jones Carrie K; Jadhav Satyawan; Weaver C David; Conn P Jeffrey; Lindsley Craig W; Niswender Colleen M^*; Hopkins Corey R

来源：Journal of Medicinal Chemistry, 2011, 54(4): 1106-1110.

DOI：10.1021/jm101271s

Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpico-linamides as positive allosteric modulators of mGlu(4). Compounds from the series show submicromolar potency at both human and rat mGlu(4). In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.

• 出版日期2011-2-24