3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.

Autor: Bernotas RC; Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Road, Collegeville, PA 19426, USA. bernotr@wyeth.com, Antane S, Shenoy R, Le VD, Chen P, Harrison BL, Robichaud AJ, Zhang GM, Smith D, Schechter LE
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Mar 01; Vol. 20 (5), pp. 1657-60. Date of Electronic Publication: 2010 Jan 21.
DOI: 10.1016/j.bmcl.2010.01.073
Abstrakt: Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT(6) receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT(6) binding affinity with K(i) values <10nM. Depending on substitution, both agonists (e.g., 6o: EC(50)=60nM, E(max)=70%) and antagonists (6y: IC(50)=17 nM, I(max)=86%) were identified in a 5-HT(6) adenylyl cyclase assay.
(Copyright 2010 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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