Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.
Bioorg Med Chem Lett
; 22(23): 7087-91, 2012 Dec 01.
Article
en En
| MEDLINE
| ID: mdl-23099092
ABSTRACT
Tyrosine ureas had been identified as potent muscarinic receptor antagonists with promising in vivo activity. Controlling the stereochemistry of the chiral quaternary ammonium center had proved to be a serious issue for this series, however. Herein we describe the preparation and SAR of tyrosine urea antagonists containing achiral quaternary ammonium centers. The most successful such moiety was the 2-methylimidazo[2,1-b][1,3]thiazol-7-ium group which yielded highly potent antagonists with long duration of action in an inhaled animal model of bronchoconstriction.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Tirosina
/
Urea
/
Receptores Muscarínicos
/
Antagonistas Muscarínicos
/
Compuestos de Amonio Cuaternario
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos