Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Bioorg Med Chem Lett
; 20(9): 2755-60, 2010 May 01.
Article
em En
| MEDLINE
| ID: mdl-20382018
ABSTRACT
Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-pyrrolidin-1-yl]-ethanone, was extensively profiled and shows promise as a potential clinical candidate.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Azepinas
/
Receptores Histamínicos H3
/
Antagonistas dos Receptores Histamínicos H3
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article