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)

被引：63
作者：
Bromidge, SM [1 ]
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
机构：
[1] SmithKline Beecham Pharmaceut, Discovery Res, Discovery Chem Europe, Harlow CM19 5AW, Essex, England
[2] SmithKline Beecham Pharmaceut, Discovery Res, Dept Drug Metab & Pharmacokinet, Harlow CM19 5AW, Essex, England
[3] SmithKline Beecham Pharmaceut, Discovery Res, Dept Neurosci Res, Harlow CM19 5AW, Essex, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 01期
关键词：
D O I：
10.1016/S0960-894X(00)00597-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2000 Elsevier Science Ltd. All rights reserved.
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页码：55 / 58
页数：4
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