N-acyloxymethyl carbamate linked prodrugs of pseudomycins are novel antifungal agents.
Bioorg Med Chem Lett
; 11(14): 1875-9, 2001 Jul 23.
Article
en En
| MEDLINE
| ID: mdl-11459651
ABSTRACT
We describe herein the synthesis, bioconversion, antifungal activity, and preliminary toxicology evaluation of a series of N-acyloxymethyl carbamate linked triprodrugs of pseudomycins. The syntheses of these prodrugs (3-6) were achieved via simple N-acylation of PSB (1) or PSC' (2) with various prodrug linkers (7-9). As expected, upon incubation with mouse and/or human plasma, many of these prodrugs (3, 5, and 6) were converted to the parent compound within a few hours. Of particular significance, two pseudomycin triprodrugs (5 and 6) showed excellent in vivo efficacy against systemic Candidiasis without tail vein irritation being observed.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Péptidos Cíclicos
/
Candidiasis
/
Profármacos
/
Antifúngicos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2001
Tipo del documento:
Article
País de afiliación:
Estados Unidos