ChemInform Abstract: 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).

Steven M. Bromidge,

Steven M. Bromidge

Dep. Discovery Chem., SmithKline Beecham Pharm., New Front. Sci. Park, Harlow, Essex CM19 5AW, UK

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et al. et al.,

et al. et al.

Dep. Discovery Chem., SmithKline Beecham Pharm., New Front. Sci. Park, Harlow, Essex CM19 5AW, UK

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Steven M. Bromidge,

Steven M. Bromidge

Dep. Discovery Chem., SmithKline Beecham Pharm., New Front. Sci. Park, Harlow, Essex CM19 5AW, UK

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et al. et al.,

et al. et al.

Dep. Discovery Chem., SmithKline Beecham Pharm., New Front. Sci. Park, Harlow, Essex CM19 5AW, UK

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First published: 27 May 2010

https://doi.org/10.1002/chin.200118134

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Abstract

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ChemInform Abstract

A variety of substituted piperazinylbenzenesulfonamides (VII) (ca. 40 examples) are prepared by parallel synthesis and evaluated for their 5-HT₆ receptor binding affinity and selectivity. Based on its overall biological profile, compound (VIIe) (SB-357134) is selected for further pre-clinical evaluation.