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ID: ALA1135108

Journal: Bioorg Med Chem Lett

Title: Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.

Authors: Bromidge SM, Clarke SE, King FD, Lovell PJ, Newman H, Riley G, Routledge C, Serafinowska HT, Smith DR, Thomas DR.

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.

CiteXplore: 11992776

DOI: 10.1016/s0960-894x(02)00172-5