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.

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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood-Brain Barrier
  • Heterocyclic Compounds
  • Indoles
  • Phenols / chemical synthesis
  • Phenols / pharmacokinetics*
  • Phenols / pharmacology
  • Protein Binding
  • Pyrrolidines / chemical synthesis
  • Pyrrolidines / pharmacokinetics*
  • Pyrrolidines / pharmacology
  • Rats
  • Receptors, Serotonin / chemistry*
  • Serotonin Antagonists / chemical synthesis*
  • Serotonin Antagonists / pharmacokinetics*
  • Serotonin Antagonists / pharmacology
  • Structure-Activity Relationship
  • Sulfonamides / pharmacokinetics

Substances

  • Heterocyclic Compounds
  • Indoles
  • Phenols
  • Pyrrolidines
  • Receptors, Serotonin
  • SB 269970
  • SB-656104-A
  • Serotonin Antagonists
  • Sulfonamides
  • serotonin 7 receptor