Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists

Bioorg Med Chem. 2009 Jul 15;17(14):5153-63. doi: 10.1016/j.bmc.2009.05.055.

Ronald C Bernotas ¹, Steven Lenicek, Schuyler Antane, Derek C Cole, Boyd L Harrison, Albert J Robichaud, Guo Ming Zhang, Deborah Smith, Brian Platt, Qian Lin, Ping Li, Joseph Coupet, Sharon Rosenzweig-Lipson, Chad E Beyer, Lee E Schechter

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Affiliation

1 Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. [email protected]

PMID: 19523834 DOI: 10.1016/j.bmc.2009.05.055

Abstract

A series of 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines 10a-z was prepared as novel 5-HT(6) ligands. The best compounds were high affinity, full agonists at 5-HT(6) receptors. Several agonists demonstrated good selectivity over Other serotonergic and dopaminergic receptors. Acute administration of selective agonist 10e significantly increased extracellular GABA concentrations in rat frontal cortex. This compound also reduced adjunctive drinking behavior in the rat schedule-induced polydipsia assay, possibly predictive of efficacy in obsessive compulsive disorder and Other anxiety related disorders.

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