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
Citation
Sm. Bromidge et al., 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), BIOORG MED, 11(1), 2001, pp. 55-58
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
1
Year of publication
2001
Pages
55 - 58
Database
ISI
SICI code
0960-894X(20010108)11:1<55:PBANAS>2.0.ZU;2-V
Abstract
Substituted N-phenyl-4-methoxy-3-piperazin-1-ylbenzenesulfonamides and conf ormationally restricted analogues have been identified as high affinity and selective 5-HT6 antagonists. Compounds from this series had a range of pha rmacokinetic 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. (C) 2000 Elsev ier Science Ltd. All rights reserved.