Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.
The synthesis and the structure activity of a new series of pyrrolo[1,2-a]pyrazine is reported. These molecules are potent and selective non-competitive mGluR5 antagonists and may shed new light on the pattern of substitution tolerated by this receptor.
Micheli
Fabrizio
F
GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming 4, 37135 Verona, Italy. fm20244@gsk.com
Bertani
Barbara
B
Bozzoli
Andrea
A
Crippa
Luca
L
Cavanni
Paolo
P
Di Fabio
Romano
R
Donati
Daniele
D
Marzorati
Paola
P
Merlo
Giancarlo
G
Paio
Alfredo
A
Perugini
Lorenzo
L
Zarantonello
Paola
P
D050483:Dopamine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors; D005453:Fluorescence; D006801:Humans; D015394:Molecular Structure; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors; D011719:Pyrazines / Q000138:chemical synthesis / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology*; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D050483:Dopamine Plasma Membrane Transport Proteins; C578935:GRM5 protein, human; D050484:Norepinephrine Plasma Membrane Transport Proteins; D011719:Pyrazines; D011758:Pyrroles; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate