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ID: ALA1134976

Journal: Bioorg Med Chem Lett

Title: SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.

Authors: Forbes IT, Douglas S, Gribble AD, Ife RJ, Lightfoot AP, Garner AE, Riley GJ, Jeffrey P, Stevens AJ, Stean TO, Thomas DR.

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.

CiteXplore: 12392747

DOI: 10.1016/s0960-894x(02)00690-x