Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
The discovery of a series of 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles, dual acting norepinephrine reuptake inhibitors (NRIs) and 5-HT(2A) receptor antagonists, is described. The synthesis and structure-activity relationship (SAR) of this novel series of compounds is also presented.
Heffernan
Gavin D
GD
Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. hefferg@wyeth.com
Coghlan
Richard D
RD
Manas
Eric S
ES
McDevitt
Robert E
RE
Li
Yanfang
Y
Mahaney
Paige E
PE
Robichaud
Albert J
AJ
Huselton
Christine
C
Alfinito
Peter
P
Bray
Jenifer A
JA
Cosmi
Scott A
SA
Johnston
Grace H
GH
Kenney
Thomas
T
Koury
Elizabeth
E
Winneker
Richard C
RC
Deecher
Darlene C
DC
Trybulski
Eugene J
EJ
D001692:Biological Transport / Q000187:drug effects; D002460:Cell Line; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D009638:Norepinephrine / Q000378:metabolism*; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D007211:Indoles; D014179:Neurotransmitter Uptake Inhibitors; D044402:Receptor, Serotonin, 5-HT2A; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists; D009638:Norepinephrine