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1: Bioorg Med Chem Lett. 2001 Jan 8;11(1):55-8.Click here to read Links

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).

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.

Discovery Chemistry Europe, SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com

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.

PMID: 11140733 [PubMed - indexed for MEDLINE]