Synthesis and in vitro evaluation of a phosphonate prodrug: bis(pivaloyloxymethyl) 9-(2-phosphonylmethoxyethyl)adenine.
Antiviral Res
; 19(3): 267-73, 1992 Sep.
Article
en En
| MEDLINE
| ID: mdl-1332606
ABSTRACT
9-(2-Phosphonylmethoxyethyl)adenine (PMEA; 1) was acylated with chloromethyl pivalate to afford bis(pivaloyloxymethyl) PMEA (2). The ester prodrug demonstrated enhanced in vitro potency against HSV-2 greater than 150-fold higher than the parent compound. The antiviral activity of 2 was 50-fold better than PMEA against HSV-1, and equipotent against HIV and HCMV. The toxicity of 2 was studied in both resting and growing cells.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Antivirales
/
Profármacos
/
Adenina
/
Organofosfonatos
Límite:
Humans
Idioma:
En
Revista:
Antiviral Res
Año:
1992
Tipo del documento:
Article