Author/Authors :
Ian T. Forbes، نويسنده , , Sara Douglas، نويسنده , , Andrew D. Gribble، نويسنده , , Robert J. Ife، نويسنده , , Andrew P. Lightfoot، نويسنده , , Ashley E. Garner، نويسنده , , Graham J. Riley، نويسنده , , Phillip Jeffrey، نويسنده , , Alexander J. Stevens، نويسنده , , Tania O. Stean، نويسنده , , David R. Thomas، نويسنده ,
Abstract :
A focused SAR study around the previously reported selective 5-HT7 receptor antagonist, SB-269970-A has resulted in the identification of a structurally related analogue having an improved pharmacokinetic profile. Replacement of the phenolic group in SB-269970-A with an indole moiety, and replacement of the piperidinyl 4-methyl group with a heterocyclic ring system proved to be the key changes leading to the identification of SB-656104-A.