1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT 6 receptor ligands

…, D Smith, J Coupet, B Harrison, LE Schechter

Index: Bernotas, Ronald; Lenicek, Steven; Antane, Schuyler; Zhang, Guo Ming; Smith, Deborah; Coupet, Joseph; Harrison, Boyd; Schechter, Lee E. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5499 - 5502

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Citation Number: 27

Abstract

Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which N, N-dimethyl-N-{2-[3-(1-naphthylsulfonyl)- 1H-indol-1-yl] ethyl} amine 8t and N-methyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl] ethyl} amine 8u showed high affinity for 5-HT6 receptors with Ki= 3.7 and 5.7 nM, respectively.