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Bioorg Med Chem Lett. 2008 Oct 15;18(20):5698-700. doi: 10.1016/j.bmcl.2008.08.010. Epub 2008 Aug 7.

Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.

Author information

  • 1Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Giancarlo.Z.Trani@gsk.com


Starting from a benzazepine sulfonamide 5-HT(6) receptor antagonist lead with limited brain penetration, application of a strategy of conformational constraint and reduction of hydrogen bond donor count led to a novel series of tricyclic derivatives with high 5-HT(6) receptor affinity and excellent brain:blood ratios.

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