1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands

Ronald C Bernotas; Schuyler A Antane; Steven E Lenicek; Simon N Haydar; Albert J Robichaud; Boyd L Harrison; Guo Ming Zhang; Deborah Smith; Joseph Coupet; Lee E Schechter

doi:10.1016/j.bmcl.2009.10.067

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6935-8. doi: 10.1016/j.bmcl.2009.10.067. Epub 2009 Oct 20.

Authors

Ronald C Bernotas¹, Schuyler A Antane, Steven E Lenicek, Simon N Haydar, Albert J Robichaud, Boyd L Harrison, Guo Ming Zhang, Deborah Smith, Joseph Coupet, Lee E Schechter

Affiliation

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

PMID: 19884004
DOI: 10.1016/j.bmcl.2009.10.067

Abstract

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines were prepared. Binding assays indicated they are 5-HT(6) receptor ligands, among which 6f and 6g showed high affinity for 5-HT(6) receptors with K(i)=3.9 and 1.7 nM, respectively.

MeSH terms

HeLa Cells
Humans
Ligands
Pyridines / chemistry
Pyridines / pharmacology*
Pyrroles / chemistry
Pyrroles / pharmacology*
Receptors, Serotonin / drug effects*
Receptors, Serotonin / metabolism
Serotonin Antagonists / chemistry
Serotonin Antagonists / pharmacology*
Serotonin Receptor Agonists / chemistry
Serotonin Receptor Agonists / pharmacology*

Substances

Ligands
Pyridines
Pyrroles
Receptors, Serotonin
Serotonin Antagonists
Serotonin Receptor Agonists
serotonin 6 receptor
pyrrolo(2, 3-b)pyridine