Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant

Title
Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
Authors
김종엽김득준강석연박우규김현정정명은손은정배애님김정민이진화
Keywords
5-HT2a; 5-HT2c; serotonin; depressant; Antidepressant; Piperazine; Pyrimidine
Issue Date
2010-11
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 20, NO 22, 6439-6442
Abstract
Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed.
URI
http://pubs.kist.re.kr/handle/201004/38351
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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