1.
Bioorg Med Chem Lett
; 18(20): 5698-700, 2008 Oct 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18793848
RESUMEN
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.