Synthesis and anti-HIV activity of cyclic pyrimidine phosphonomethoxy nucleosides and their prodrugs: a comparison of phosphonates and corresponding nucleosides.
Nucleosides Nucleotides Nucleic Acids
; 26(6-7): 573-7, 2007.
Article
em En
| MEDLINE
| ID: mdl-18066858
ABSTRACT
Cyclic phosphonomethoxy pyrimidine nucleosides that are bioisosteres of the monophosphate metabolites of HIV reverse transcriptase (RT) inhibitors AZT, d4T, and ddC have been synthesized. The RT inhibitory activities of the phosphonates were reduced for both dideoxy (dd) and dideoxydidehydro (d4) analogs compared to the nucleosides. Bis-isopropyloxymethylcarbonyl (BisPOC) prodrugs were prepared on selected compounds and provided > 150-fold improvements in antiviral activity.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pró-Fármacos
/
Fármacos Anti-HIV
/
Organofosfonatos
/
Nucleosídeos
Idioma:
En
Revista:
Nucleosides Nucleotides Nucleic Acids
Ano de publicação:
2007
Tipo de documento:
Article