4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands.
The preparation of a novel class of 4-(2-aminoethoxy)-N-(phenylsulfonyl)indoles which exhibit high affinity towards the 5-HT6 receptor is reported here. Among these compounds, 4-(2-methylaminoethoxy)-N-(phenylsulfonyl)indole 5g showed superior affinity (Ki = 1 nM) towards the 5-HT6 receptor as well as excellent selectivity (> 2000-fold) against the closely related subtype 5-HT7 receptor.
Zhou
Ping
P
Chemical and Screening Science and Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. zhoup@wyeth.com
Yan
Yinfa
Y
Bernotas
Ronald
R
Harrison
Boyd L
BL
Huryn
Donna
D
Robichaud
Albert J
AJ
Zhang
Guo Ming
GM
Smith
Deborah L
DL
Schechter
Lee E
LE
D001667:Binding, Competitive; D007211:Indoles / Q000138:chemical synthesis / Q000145:classification / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D011985:Receptors, Serotonin / Q000187:drug effects*; D013329:Structure-Activity Relationship
D007211:Indoles; D008024:Ligands; D011985:Receptors, Serotonin; C097216:serotonin 6 receptor