The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate

[Display omitted] •First description of the SAR that led to the discovery of VU2957 (Valiglurax).•Valiglurax is only the second mGlu4 PAM clinical candidate for Parkinson’s disease.•The new series afford improvements in protein binding, half-life in vivo, CNS penetration and oral bioavailability.•Hi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2019-01, Vol.29 (2), p.342-346
Hauptverfasser:	Panarese, Joseph D., Engers, Darren W., Wu, Yong-Jin, Guernon, Jason M., Chun, Aspen, Gregro, Alison R., Bender, Aaron M., Capstick, Rory A., Wieting, Joshua M., Bronson, Joanne J., Macor, John E., Westphal, Ryan, Soars, Matthew, Engers, Julie E., Felts, Andrew S., Rodriguez, Alice L., Emmitte, Kyle A., Jones, Carrie K., Blobaum, Anna L., Jeffrey Conn, P., Niswender, Colleen M., Hopkins, Corey R., Lindsley, Craig W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Metabotropic glutamate receptor mGlu4 Parkinson’s disease (PD) Positive allosteric modulator (PAM) Structure-activity relationship (SAR)
Online-Zugang:	Volltext
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