1330626-14-6Relevant articles and documents
Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4)
Engers, Darren W.,Blobaum, Anna L.,Gogliotti, Rocco D.,Cheung, Yiu-Yin,Salovich, James M.,Garcia-Barrantes, Pedro M.,Daniels, J. Scott,Morrison, Ryan,Jones, Carrie K.,Soars, Matthew G.,Zhuo, Xiaoliang,Hurley, Jeremy,Macor, John E.,Bronson, Joanne J.,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
, p. 1192 - 1200 (2016)
The efficacy of positive allosteric modulators (PAMs) of the metabotropic glutamate receptor 4 (mGlu4) in preclinical rodent models of Parkinson's disease has been established by a number of groups. Here, we report an advanced preclinically characterized mGlu4 PAM, N-(3-chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506). We detail the discovery of VU0418506 starting from a common picolinamide core scaffold and evaluation of a number of amide bioisosteres leading to the novel pyrazolo[4,3-b]pyridine head group. VU0418506 has been characterized as a potent and selective mGlu4 PAM with suitable in vivo pharmacokinetic properties in three preclinical safety species.
