Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363364 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT6 receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT6 binding affinity with Ki values <10 nM. Depending on substitution, both agonists (e.g., 6o: EC50 = 60 nM, Emax = 70%) and antagonists (6y: IC50 = 17 nM, Imax = 86%) were identified in a 5-HT6 adenylyl cyclase assay.
Graphical abstractA series of 1-(azacyclyl)-3-arylsulfonyl-1H-indoles 6 was prepared as constrained 5-HT6 modulators.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Ronald C. Bernotas, Schuyler Antane, Rajesh Shenoy, Van-Duc Le, Ping Chen, Boyd L. Harrison, Albert J. Robichaud, Guo Ming Zhang, Deborah Smith, Lee E. Schechter,