The Design and Synthesis of 1,4-Substituted Piperazine Derivatives as Triple Reuptake Inhibitors

Title
The Design and Synthesis of 1,4-Substituted Piperazine Derivatives as Triple Reuptake Inhibitors
Authors
한민수한영휘송치만한호규
Keywords
antidepression; CNS drug; piperazine; Major depressive disorder; Antidepressants; Triple reuptake inhibitor
Issue Date
2012-08
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 33, NO 8, 2597-2602
Abstract
Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.
URI
http://pubs.kist.re.kr/handle/201004/43132
ISSN
02532964
Appears in Collections:
KIST Publication > Article
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE