Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.
Bioorg Med Chem Lett
; 20(2): 618-22, 2010 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-20006499
ABSTRACT
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa inhibitors, incorporating neutral and basic monoaryl P4 groups, ultimately producing potent inhibitors with effective levels of anticoagulant activity and extended oral pharmacokinetic profiles. However, time dependant inhibition of Cytochrome P450 3A4 was a particular issue with this series.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinonas
/
Fator X
/
Anticoagulantes
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Reino Unido