Design and synthesis of novel series of 5-HT6 receptor ligands having indole, a central aromatic core and 1-amino-4 methyl piperazine as a positive ionizable group.
Bioorg Med Chem
; 21(17): 5573-82, 2013 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-23810425
ABSTRACT
The exclusive distribution of 5-HT6 receptor in the brain regions and high affinity for antipsychotic and antidepressant drugs makes 5-HT6 receptor a promising target in treatment of CNS diseases. Based on a pharmacophore model reported in the literature, we designed and synthesized a novel series of 5-HT6 receptor ligands having indole as a central aromatic core and 1-amino-4-methyl piperazine as positive ionizable group. Out of 32 compounds we have successfully identified 10 new compounds as 5-HT6 receptor antagonists. The structure-activity relationship (SAR) studies have been carried out by mapping the compounds with the 3D QSAR model.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
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Antagonistas da Serotonina
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Desenho de Fármacos
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Receptores de Serotonina
/
Indóis
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2013
Tipo de documento:
Article