An article The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu(4) PAM development candidate WOS:000454616600043 published article about POSITIVE ALLOSTERIC MODULATOR; MGLUR4; VU0418506; SERIES in [Panarese, Joseph D.; Engers, Darren W.; Chun, Aspen; Gregro, Alison R.; Bender, Aaron M.; Capstick, Rory A.; Wieting, Joshua M.; Engers, Julie E.; Felts, Andrew S.; Rodriguez, Alice L.; Emmitte, Kyle A.; Jones, Carrie K.; Blobaum, Anna L.; Conn, P. Jeffrey; Niswender, Colleen M.; Hopkins, Corey R.; Lindsley, Craig W.] Vanderbilt Univ, Vanderbilt Ctr Neurosci Drug Discovery, Nashville, TN 37232 USA; [Panarese, Joseph D.; Engers, Darren W.; Chun, Aspen; Gregro, Alison R.; Bender, Aaron M.; Capstick, Rory A.; Wieting, Joshua M.; Engers, Julie E.; Felts, Andrew S.; Rodriguez, Alice L.; Emmitte, Kyle A.; Jones, Carrie K.; Blobaum, Anna L.; Conn, P. Jeffrey; Niswender, Colleen M.; Hopkins, Corey R.; Lindsley, Craig W.] Vanderbilt Univ, Dept Pharmacol, Nashville, TN 37232 USA; [Wu, Yong-Jin; Guernon, Jason M.; Bronson, Joanne J.; Macor, John E.; Westphal, Ryan; Soars, Matthew] Bristol Myers Squibb Co, Res & Dev, 5 Res Pkwy, Wallingford, CT 06492 USA; [Lindsley, Craig W.] Vanderbilt Univ, Dept Chem, Nashville, TN 37232 USA; [Lindsley, Craig W.] Vanderbilt Univ, Dept Biochem, Nashville, TN 37232 USA; [Conn, P. Jeffrey; Niswender, Colleen M.] Vanderbilt Univ, Med Ctr, Vanderbilt Kennedy Ctr, Nashville, TN 37232 USA in 2019.0, Cited 18.0. The Name is 3,5-Dimethyl-1H-pyrazole. Through research, I have a further understanding and discovery of 67-51-6. COA of Formula: C5H8N2
This letter describes the first account of the chemical optimization (SAR and DMPK profiling) of a new series of mGlu(4) positive allosteric modulators (PAMs), leading to the identification of VU0652957 (VU2957, Valiglurax), a compound profiled as a preclinical development candidate. Here, we detail the challenges faced in allosteric modulator programs (e.g., steep SAR, as well as subtle structural changes affecting overall physiochemical/DMPK properties and CNS penetration).
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Reference:
Pyrazole – Wikipedia,
,Pyrazoles – an overview | ScienceDirect Topics