Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.
Norepinephrine and serotonin play an important role in a wide variety of biological processes and are implicated in a number of neurological disorders. A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones was designed and synthesized that displays potent norepinephrine reuptake inhibition while maintaining high selectivity (>100-fold) against the human serotonin and dopamine transporters.
McComas
Casey C
CC
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, S2227A, Collegeville, PA 19426, USA. mccomac@wyeth.com
Vu
An T
AT
Mahaney
Paige E
PE
Cohn
Stephen T
ST
Fensome
Andrew
A
Marella
Michael A
MA
Nogle
Lisa
L
Trybulski
Eugene J
EJ
Ye
Fei
F
Zhang
Puwen
P
Alfinito
Peter
P
Bray
Jenifer
J
Johnston
Grace
G
Koury
Elizabeth
E
Deecher
Darlene C
DC
D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009638:Norepinephrine / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D007211:Indoles; D014179:Neurotransmitter Uptake Inhibitors; C456900:indolin-2-one; D009638:Norepinephrine