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Bioorg Med Chem Lett. 2002 Nov 18;12(22):3341-4.

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

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  • 1GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK.


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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