Orally active factor Xa inhibitor: synthesis and biological activity of masked amidines as prodrugs of novel 1,4-diazepane derivatives.
Bioorg Med Chem
; 12(20): 5415-26, 2004 Oct 15.
Article
en En
| MEDLINE
| ID: mdl-15388168
ABSTRACT
Factor Xa (fXa) is a serine protease, which plays a pivotal role in the coagulation cascade. To improve the oral anticoagulant activity of fXa inhibitors containing a 1,4-diazepane moiety as the P4 part, a prodrug strategy was examined. Among the compounds evaluated in this study, amidoxime prodrugs bearing an ester moiety, such as compounds 21 and 30, showed effective oral anticoagulant activity in mice.
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Bases de datos:
MEDLINE
Asunto principal:
Profármacos
/
Antitrombina III
/
Amidinas
/
Anticoagulantes
Límite:
Animals
/
Female
/
Humans
/
Pregnancy
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Japón