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

ID: ALA1144232

Journal: Bioorg Med Chem Lett

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

Authors: Trani G, Baddeley SM, Briggs MA, Chuang TT, Deeks NJ, Johnson CN, Khazragi AA, Mead TL, Medhurst AD, Milner PH, Quinn LP, Ray AM, Rivers DA, Stean TO, Stemp G, Trail BK, Witty DR.

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.

CiteXplore: 18793848

DOI: 10.1016/j.bmcl.2008.08.010

Patent ID: ┄