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SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties |
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| Authors: | Forbes Ian T Douglas Sara Gribble Andrew D Ife Robert J Lightfoot Andrew P Garner Ashley E Riley Graham J Jeffrey Phillip Stevens Alexander J Stean Tania O Thomas David R |
| Affiliation: | GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. ian_t_forbes@gsk.com |
| Abstract: | A focused SAR study around the previously reported selective 5-HT(7) 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. |
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