Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
Bioorg Med Chem Lett
; 13(2): 191-6, 2003 Jan 20.
Article
en En
| MEDLINE
| ID: mdl-12482421
ABSTRACT
A highly potent water soluble triazole antifungal prodrug, RO0098557 (1), has been identified from its parent, the novel antifungal agent RO0094815 (2). The prodrug includes a triazolium salt linked to an aminocarboxyl moiety, which undergoes enzymatic activation followed by spontaneous chemical degradation to release 2. Prodrug 1 showed high chemical stability and water solubility and exhibited strong antifungal activity against systemic candidiasis and aspergillosis as well as pulmonary aspergillosis in rats.
Buscar en Google
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Triazoles
/
Profármacos
/
Antifúngicos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2003
Tipo del documento:
Article
País de afiliación:
Japón