Antiviral nucleoside drug delivery via amino acid phosphoramidates.

Antiviral nucleoside drug delivery via amino acid phosphoramidates.
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DOI:
10.1080/15257779908041599
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发表时间:
1999-04
期刊:
Nucleosides & nucleotides
影响因子:
--
通讯作者:
C. Wagner;S. Chang;G. Griesgraber;Heng Song;E. McIntee;C. Zimmerman
C. Wagner;S. Chang;G. Griesgraber;Heng Song;E. McIntee;C. Zimmerman
中科院分区:
其他
文献类型:
--
作者:
C. Wagner;S. Chang;G. Griesgraber;Heng Song;E. McIntee;C. Zimmerman

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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.