95539-67-6Relevant articles and documents
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT6 receptor modulators
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.
scheme or table, p. 1657 - 1660 (2010/07/03)
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 50 = 60 nM, Emax = 70%) and antagonists (6y: IC50 = 17 nM, Imax = 86%) were identified in a 5-HT6 adenylyl cyclase assay.
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands
Bernotas, Ronald,Lenicek, Steven,Antane, Schuyler,Zhang, Guo Ming,Smith, Deborah,Coupet, Joseph,Harrison, Boyd,Schechter, Lee E.
, p. 5499 - 5502 (2007/10/03)
Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which N,N-dimethyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8t and N-methyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8u showed high affinity for 5-HT6 receptors with Ki = 3.7 and 5.7 nM, respectively. Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which N,N-dimethyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8t and N-methyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8u showed high affinity for 5-HT6 receptors with Ki = 3.7 and 5.7 nM, respectively.
A Facile Synthesis of 3-Sulfonyl-Substituted Indole Derivatives
Wojciechowski, Krzysztof,Makosza, Mieczyslaw
, p. 651 - 653 (2007/10/02)
A new method for the synthesis of 3-sulfonyl-substituted indole derivatives 5 was developed starting from the easily available products of the vicarious nucleophilic substitution of hydrogen in nitroarenes 1.