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

…, P Chen, BL Harrison, AJ Robichaud, GM Zhang…

Index: Bernotas, Ronald C.; Antane, Schuyler; Shenoy, Rajesh; Le, Van-Duc; Chen, Ping; Harrison, Boyd L.; Robichaud, Albert J.; Zhang, Guo Ming; Smith, Deborah; Schechter, Lee E. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 5 p. 1657 - 1660

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Citation Number: 11

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< 10nM. Depending on substitution, both agonists (eg, 6o: EC50= 60nM, Emax= 70%) and antagonists (6y: IC50= 17 nM, Imax= 86%) were identified in a 5-HT6 adenylyl cyclase ...