Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.
Bioorg Med Chem Lett
; 20(17): 5069-73, 2010 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-20674357
ABSTRACT
A novel imidazobenzazepine template (5a) with potent dual H(1)/5-HT(2A) antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R(1)-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]-2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H(1)/5-HT(2A) receptor antagonist activities and good developability profiles.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Antagonistas da Serotonina
/
Transtornos do Sono-Vigília
/
Receptor 5-HT1A de Serotonina
/
Receptor 5-HT2A de Serotonina
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article