Authors Panarese, JD; Engers, DW; Wu, YJ; Guernon, JM; Chun, A; Gregro, AR; Bender, AM; Capstick, RA; Wieting, JM; Bronson, JJ; Macor, JE; Westphal, R; Soars, M; Engers, JE; Felts, AS; Rodriguez, AL; Emmitte, KA; Jones, CK; Blobaum, AL; Conn, PJ; Niswender, CM; Hopkins, CR; Lindsley, CW in PERGAMON-ELSEVIER SCIENCE LTD 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. Application In Synthesis of 3,5-Dimethyl-1H-pyrazole. The Name is 3,5-Dimethyl-1H-pyrazole. Through research, I have a further understanding and discovery of 67-51-6
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