Portal de Periódicos da CAPES

Antiviral Nucleoside Drug Delivery via Amino Acid Phosphoramidates

1999; Taylor & Francis; Volume: 18; Issue: 4-5 Linguagem: Inglês

10.1080/15257779908041599

2332-3892

Carston R. Wagner, Shu-Ling Chang, George Griesgraber, Heng Song, Edward J. McIntee, Cheryl L. Zimmerman,

Click Chemistry and Applications

Abstract Stable and water soluble amino acid phosphomonoester amidates of AZT were synthesized and shown to have potent anti-HIV-1 activity. Intracellular and cell extract metabolism studies revealed that these compounds are likely to be enzymatically converted to the corresponding monophosphates. In addition, we have shown that the half life and tissue distribution of a phosphoramidate of AZT is 5 and 10-fold greater, respectively, than AZT.