From pyrroles to pyrrolo[1,2-a]pyrazinones: a new class of mGluR1 antagonists.
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.
Micheli
Fabrizio
F
GlaxoSmithKline Medicine Research Centre, Via Fleming,4, 37135 Verona, Italy. Fabrizio.E.Micheli@gsk.com
Cavanni
Paolo
P
Di Fabio
Romano
R
Marchioro
Carla
C
Donati
Daniele
D
Faedo
Stefania
S
Maffeis
Micaela
M
Sabbatini
Fabio Maria
FM
Tranquillini
Maria Elvira
ME
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
D011719:Pyrazines; D011758:Pyrroles; D018094:Receptors, Metabotropic Glutamate; C104077:metabotropic glutamate receptor type 1