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Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists |
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| Authors: | Trani Giancarlo Baddeley Stuart M Briggs Michael A Chuang Tsu T Deeks Nigel J Johnson Christopher N Khazragi Abir A Mead Tania L Medhurst Andrew D Milner Peter H Quinn Leann P Ray Alison M Rivers Dean A Stean Tania O Stemp Geoffrey Trail Brenda K Witty David R |
| Affiliation: | Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Giancarlo.Z.Trani@gsk.com |
| Abstract: | 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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