Synthesis and anti-HIV activity of prodrugs of azidothymidine

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Abstract

In order to enhance the therapeutic efficacy of azidothymidine (AZT) by improving its pharmacokinetic properties, three prodrugs of AZT were synthesized by esterifying the 5'-hydroxyl of AZT with three pharmacologically inactive steroidal 17β-carboxylic acids. Preliminary results of in vitro anti-HIV activity screening of the compounds show that all of these esters have anti-HIV activity comparable to that of AZT. This report discusses the synthesis and anti-HIV activity screening results of the prodrugs.

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Sharma, A. P., Ollapally, A. P., & Lee, H. J. (1993). Synthesis and anti-HIV activity of prodrugs of azidothymidine. Antiviral Chemistry and Chemotherapy, 4(2), 93–96. https://doi.org/10.1177/095632029300400203

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