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

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

  • Bioorg Med Chem Lett. 2002 Nov 18;12(22):3341-4. doi: 10.1016/s0960-894x(02)00690-x.
Ian T Forbes 1,  Sara Douglas,  Andrew D Gribble,  Robert J Ife,  Andrew P Lightfoot,  Ashley E Garner,  Graham J Riley,  Phillip Jeffrey,  Alexander J Stevens,  Tania O Stean,  David R Thomas
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Affiliation

PMID: 12392747 DOI: 10.1016/s0960-894x(02)00690-x
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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