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：64

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.

引用

页码：55 / 58

页数：4

共 6 条

[1] 5-HT6 receptors as emerging targets for drug discovery [J].