Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.
Bioorg Med Chem Lett
; 20(22): 6439-42, 2010 Nov 15.
Article
em En
| MEDLINE
| ID: mdl-20933409
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
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Pirimidinas
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Antidepressivos de Segunda Geração
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Receptor 5-HT2A de Serotonina
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Receptor 5-HT2C de Serotonina
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Proteínas da Membrana Plasmática de Transporte de Serotonina
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Amidas
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article