Abstract
The synthesis of novel 3-(octahydropyrido[1,2-a]pyrazin-2-yl)- and 3-(hexahydropyrrolo[1,2-a]pyrazin-2-yl)phenyl-2-benzo[b]thiophene sulphonamide derivatives 3, (S)-4 and (R)-4 is described. The compounds show high affinity for the 5-HT6 receptor, excellent selectivity against a range of other receptors and good brain penetration.
MeSH terms
-
Drug Design
-
Kinetics
-
Models, Molecular
-
Molecular Conformation
-
Piperazines / chemical synthesis*
-
Piperazines / pharmacology
-
Receptors, Serotonin / drug effects
-
Receptors, Serotonin / metabolism*
-
Serotonin Antagonists / chemical synthesis*
-
Serotonin Antagonists / pharmacology
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis*
-
Sulfonamides / pharmacology
Substances
-
Piperazines
-
Receptors, Serotonin
-
Serotonin Antagonists
-
Sulfonamides