Discovery of a Potent, Selective, and Orally Active Phosphodiesterase 10A Inhibitor for the Potential Treatment of Schizophrenia

We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited selectivity versus the other phosphodiesterases (PD...

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Veröffentlicht in:	Journal of medicinal chemistry 2014-05, Vol.57 (10), p.4196-4212
Hauptverfasser:	Bartolomé-Nebreda, José Manuel, Delgado, Francisca, Martín-Martín, María Luz, Martínez-Viturro, Carlos M, Pastor, Joaquín, Tong, Han Min, Iturrino, Laura, Macdonald, Gregor J, Sanderson, Wendy, Megens, Anton, Langlois, Xavier, Somers, Marijke, Vanhoof, Greet, Conde-Ceide, Susana
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Drug Discovery High-Throughput Screening Assays Phosphodiesterase Inhibitors - chemical synthesis Phosphodiesterase Inhibitors - pharmacology Phosphodiesterase Inhibitors - therapeutic use Phosphoric Diester Hydrolases - drug effects Rats Schizophrenia - drug therapy Structure-Activity Relationship
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