Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.
Within the continuous quest for the discovery of novel compounds able to treat anxiety and depression, the generation of a pharmacophore model for 5-HT2C receptor antagonists and the discovery of a new class of potent and selective 5-HT2C molecules are reported.
Micheli
Fabrizio
F
GlaxoSmithKline Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy. fm20244@gsk.com
Pasquarello
Alessandra
A
Tedesco
Giovanna
G
Hamprecht
Dieter
D
Bonanomi
Giorgio
G
Checchia
Anna
A
Jaxa-Chamiec
Albert
A
Damiani
Federica
F
Davalli
Silvia
S
Donati
Daniele
D
Gallotti
Chiara
C
Petrone
Marcella
M
Rinaldi
Marilisa
M
Riley
Graham
G
Terreni
Silvia
S
Wood
Martyn
M
D008958:Models, Molecular; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011760:Pyrrolidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*
D011758:Pyrroles; D011760:Pyrrolidinones; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists