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ID: ALA1134050
Journal: Bioorg Med Chem Lett
Title: Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Authors: Bromidge SM, Clarke SE, Gager T, Griffith K, Jeffrey P, Jennings AJ, Joiner GF, King FD, Lovell PJ, Moss SF, Newman H, Riley G, Rogers D, Routledge C, Serafinowska H, Smith DR.
Abstract: Substituted N-phenyl-4-methoxy-3-piperazin-1-ylbenzenesulfonamides and conformationally restricted analogues have been identified as high affinity and selective 5-HT6 antagonists. Compounds from this series had a range of pharmacokinetic profiles in rat and in general there was a correlation between clearance and CNS penetration. Based on its overall biological profile 2 (SB-357134) was selected for further pre-clinical evaluation.
CiteXplore: 11140733