2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression.
Recently a class of compounds known as triple reuptake inhibitors has emerged as a new strategy for the treatment of depression. These compounds work by simultaneously inhibiting the synaptic reuptake of serotonin, norepinephrine and dopamine. In this Letter we describe the optimization of a novel series of 2-substituted N-aryl piperazine based triple reuptake inhibitors.
Carter
David S
DS
Department of Medicinal Chemistry, Roche Palo Alto LLC, CA 94304, USA. david.carter5@comcast.net
Cai
Hai-Ying
HY
Lee
Eun Kyung
EK
Iyer
Pravin S
PS
Lucas
Matthew C
MC
Roetz
Ralf
R
Schoenfeld
Ryan C
RC
Weikert
Robert J
RJ
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003863:Depression / Q000188:drug therapy*; D004298:Dopamine / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D051379:Mice; D015394:Molecular Structure; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009638:Norepinephrine / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012701:Serotonin / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013569:Synapses / Q000187:drug effects / Q000378:metabolism
D000928:Antidepressive Agents; D014179:Neurotransmitter Uptake Inhibitors; D010879:Piperazines; D012701:Serotonin; D004298:Dopamine; D009638:Norepinephrine