Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists.
Bioorg Med Chem
; 23(6): 1313-20, 2015 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-25684421
ABSTRACT
A novel series of 4-nitroindole sulfonamides containing a methyleneamino-N,N-dimethylformamidine were prepared. The binding of these compounds to 5-HT2A and 5-HT2C was evaluated, and most of the compounds showed IC50 values of less than 1µM, and exhibited high selectivity for the 5-HT2C receptor. However, little selectivity was observed in the functional assay for 5-HT6 receptors. The computational modeling studies further validated the biological results and also demonstrated a reasonable correlation between the activity of compounds and the mode of superimposition with specified pharmacophoric features.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptor 5-HT2A de Serotonina
/
Antagonistas do Receptor 5-HT2 de Serotonina
/
Indóis
/
Nitrocompostos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article