Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines.
Bioorg Med Chem Lett
; 18(19): 5303-6, 2008 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-18782666
ABSTRACT
A series of thio-alkyl containing diphenylethers were designed and evaluated, as a strategy to competitively direct metabolism away from unwanted amine N-demethylation and deliver a pharmacologically inactive S-oxide metabolite. Overall, sulfonamide 20 was found to possess the best balance of target pharmacology, pharmacokinetics and metabolism profile.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Éteres Fenílicos
/
Sulfonamidas
/
Benzilaminas
/
Inibidores Seletivos de Recaptação de Serotonina
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Reino Unido