The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.
Bioorg Med Chem Lett
; 20(9): 2916-9, 2010 May 01.
Article
em En
| MEDLINE
| ID: mdl-20347297
ABSTRACT
A series of 2-(3-aminopiperidine)-benzimidazoles were identified as selective H(1)-antihistamines for evaluation as potential sedative hypnotics. Representative compounds showed improved hERG selectivity over a previously identified 2-aminobenzimidazole series. While hERG activity could be modulated via manipulation of the benzimidazole N1 substituent, this approach led to a reduction in CNS exposure for the more selective compounds. One example, 9q, retained a suitable selectivity profile with CNS exposure equivalent to known centrally active H(1)-antihistamines.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Benzimidazóis
/
Sistema Nervoso Central
/
Antagonistas dos Receptores Histamínicos H1
/
Distúrbios do Início e da Manutenção do Sono
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article