SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Forbes IT,
Douglas S,
Gribble AD,
Ife RJ,
Lightfoot AP,
Garner AE,
Riley GJ,
Jeffrey P,
Stevens AJ,
Stean TO,
Thomas DR.
GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. ian_t_forbes@gsk.com
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.
PMID: 12392747 [PubMed - indexed for MEDLINE]