Antiviral Nucleoside Drug Delivery via Amino Acid Phosphoramidates |
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| Authors: | Carston R. Wagner Shu-Ling Chang George W. Griesgraber Heng Song Edward J. McIntee Cheryl L. Zimmerman |
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| Affiliation: | 1. Department of Medicinal Chemistry , University of Minnesota , Minneapolis, MN, 55455;2. Department of Pharmaceutics , College of Pharmacy, University of Minnesota , Minneapolis, MN, 55455 |
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| Abstract: | ![]()
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. |
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