New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.
The synthesis and the SAR of a new series of potent and selective dopamine D(3) receptor antagonists is reported. The new scaffolds of the [g]-fused and the hetero-fused tricyclic benzazepine are here reported together with their pharmacokinetic profile.
Micheli
Fabrizio
F
GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy. fm20244@gsk.com
Bonanomi
Giorgio
G
Braggio
Simone
S
Capelli
Anna Maria
AM
Damiani
Federica
F
Di Fabio
Romano
R
Donati
Daniele
D
Gentile
Gabriella
G
Hamprecht
Dieter
D
Perini
Ornella
O
Petrone
Marcella
M
Tedesco
Giovanna
G
Terreni
Silvia
S
Worby
Angela
A
Heidbreder
Christian
C
D000818:Animals; D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D015394:Molecular Structure; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D001552:Benzazepines; D018492:Dopamine Antagonists; D050637:Receptors, Dopamine D3