Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.
Bioorg Med Chem Lett
; 22(23): 7087-91, 2012 Dec 01.
Article
em 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
Base de dados:
MEDLINE
Assunto principal:
Tirosina
/
Ureia
/
Receptores Muscarínicos
/
Antagonistas Muscarínicos
/
Compostos de Amônio Quaternário
Limite:
Animals
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article