Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
A series of heterocyclic cycloalkanol ethylamines have been prepared to expand our norepinephrine reuptake inhibitor (NRI) program. Synthesis of a variety of heterocycles identified (+)-S-21, a potent NRI efficacious in an animal model for thermoregulatory dysfunction.
Sabatucci
Joseph P
JP
Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. sabatuj@wyeth.com
Mahaney
Paige E
PE
Leiter
Jennifer
J
Johnston
Grace
G
Burroughs
Kevin
K
Cosmi
Scott
S
Zhang
Yingru
Y
Ho
Douglas
D
Deecher
Darlene C
DC
Trybulski
Eugene
E
D000818:Animals; D018360:Crystallography, X-Ray; D005021:Ethylamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008968:Molecular Conformation; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D009638:Norepinephrine / Q000737:chemistry / Q000378:metabolism*; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D005021:Ethylamines; D014179:Neurotransmitter Uptake Inhibitors; D010879:Piperazines; D013876:Thiophenes; D009638:Norepinephrine