title: From pyrroles to pyrrolo[1,2-a]pyrazinones: a new class of mGluR1 antagonists.
abstract: 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.
authors.affiliation: GlaxoSmithKline Medicine Research Centre, Via Fleming,4, 37135 Verona, Italy. Fabrizio.E.Micheli@gsk.com
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Micheli
authors.forename: Paolo
authors.initials: P
authors.lastname: Cavanni
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Carla
authors.initials: C
authors.lastname: Marchioro
authors.forename: Daniele
authors.initials: D
authors.lastname: Donati
authors.forename: Stefania
authors.initials: S
authors.lastname: Faedo
authors.forename: Micaela
authors.initials: M
authors.lastname: Maffeis
authors.forename: Fabio Maria
authors.initials: FM
authors.lastname: Sabbatini
authors.forename: Maria Elvira
authors.initials: ME
authors.lastname: Tranquillini
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011719:Pyrazines / Q000737:chemistry* / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry*; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D011719:Pyrazines; D011758:Pyrroles; D018094:Receptors, Metabotropic Glutamate; C104077:metabotropic glutamate receptor type 1