1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands

Ronald Bernotas; Steven Lenicek; Schuyler Antane; Guo Ming Zhang; Deborah Smith; Joseph Coupet; Boyd Harrison; Lee E Schechter

doi:10.1016/j.bmcl.2004.09.003

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5499-502. doi: 10.1016/j.bmcl.2004.09.003.

Authors

Ronald Bernotas¹, Steven Lenicek, Schuyler Antane, Guo Ming Zhang, Deborah Smith, Joseph Coupet, Boyd Harrison, Lee E Schechter

Affiliation

¹ Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. bernotr@wyeth.com

PMID: 15482912
DOI: 10.1016/j.bmcl.2004.09.003

Abstract

Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT(6) 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-HT(6) receptors with K(i)=3.7 and 5.7 nM, respectively.

MeSH terms

Amines / chemical synthesis
Amines / pharmacology
Binding, Competitive
HeLa Cells
Humans
Indoles / chemical synthesis*
Indoles / pharmacology*
Ligands
Molecular Structure
Receptors, Serotonin / drug effects*
Receptors, Serotonin / physiology
Structure-Activity Relationship

Substances

Amines
Indoles
Ligands
Receptors, Serotonin
serotonin 6 receptor