Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
J Med Chem
; 45(25): 5415-8, 2002 Dec 05.
Article
em En
| MEDLINE
| ID: mdl-12459007
ABSTRACT
In search of a backup M(2) muscarinic receptor antagonist to the previously reported compound 1, we discovered compound (+)-14, which showed superior oral efficacy in animal models. The improvement of oral efficacy was achieved by modulating both the molecular weight and lipophilicity of the lead compounds.
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Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Fármacos do Sistema Nervoso Central
/
Receptores Muscarínicos
/
Autorreceptores
/
Antagonistas Muscarínicos
Idioma:
En
Ano de publicação:
2002
Tipo de documento:
Article