From pyrroles to pyrrolo[1,2- a]pyrazinones: A new class of mGluR1 antagonists

A new class of mGluR1 noncompetitive antagonists is reported. Exploiting the SAR of the known pyrrole derivatives, a new class of mGluR1 antagonists was developed through a cyclization of the C-2 position on the pyrrole N-1 nitrogen. The resulting pyrrolo[1,2- a]pyrazinones are potent and noncompeti...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-03, Vol.16 (5), p.1342-1345
Hauptverfasser:	Micheli, Fabrizio, Cavanni, Paolo, Di Fabio, Romano, Marchioro, Carla, Donati, Daniele, Faedo, Stefania, Maffeis, Micaela, Sabbatini, Fabio Maria, Tranquillini, Maria Elvira
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antagonist Biological and medical sciences CHO Cells Cricetinae Excitatory amino acids Glutamatergic system (aspartate and other excitatory aminoacids) Inhibitory Concentration 50 Medical sciences Metabotropic mGluR1 Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyrazines - chemistry Pyrazines - pharmacology Pyrrole Pyrroles - chemistry Receptors, Metabotropic Glutamate - antagonists & inhibitors Receptors, Metabotropic Glutamate - metabolism Structure-Activity Relationship
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Zusammenfassung:	A new class of mGluR1 noncompetitive antagonists is reported. Exploiting the SAR of the known pyrrole derivatives, a new class of mGluR1 antagonists was developed through a cyclization of the C-2 position on the pyrrole N-1 nitrogen. The resulting pyrrolo[1,2- a]pyrazinones are potent and noncompetitive antagonists.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.11.049