Structure-based optimization of a potent class of arylamide FMS inhibitors.
Bioorg Med Chem Lett
; 18(12): 3632-7, 2008 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-18495479
ABSTRACT
An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replacement groups. Structure-based modeling provided the framework to efficiently effect this transformation and restore potencies to previous levels. This optimization removed a risk factor for potential idiosyncratic drug reactions.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fenilenodiaminas
/
Desenho de Fármacos
/
Receptor de Fator Estimulador de Colônias de Macrófagos
/
Inibidores Enzimáticos
/
Anti-Inflamatórios
Tipo de estudo:
Prognostic_studies
/
Risk_factors_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Estados Unidos