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Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists
Steven M Bromidge1, Stephen E Clarke, Frank D King
1Department of Psychiatry, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK.
Bioorganic & Medicinal Chemistry Letters
|May 7, 2002
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.