Identification of novel NK₁/NK₃ dual antagonists for the potential treatment of schizophrenia

During the lead optimization of NK₁/NK₃ receptor antagonists program, a focused exploration of molecules bearing a lactam moiety was performed. The aim of the investigation was to identify the optimal position of the carbonyl and hydroxy methyl group in the lactam moiety, in order to maximize the in...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (22), p.6899-6904
Hauptverfasser:	Catalani, Maria Pia, Alvaro, Giuseppe, Bernasconi, Giovanni, Bettini, Ezio, Bromidge, Steven M, Heer, Jag, Tedesco, Giovanna, Tommasi, Simona
Format:	Artikel
Sprache:	eng
Schlagworte:	antagonists Antipsychotic Agents - chemistry Antipsychotic Agents - pharmacology Biological and medical sciences Humans Lactams - chemistry Lactams - pharmacology Medical sciences Models, Molecular Neurokinin-1 Receptor Antagonists Pharmacology. Drug treatments receptors Receptors, Neurokinin-1 - metabolism Receptors, Neurokinin-3 - antagonists & inhibitors Receptors, Neurokinin-3 - metabolism schizophrenia Schizophrenia - drug therapy Structure-Activity Relationship
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