6-substituted derivatives of carbovir: Anti-HIV activity

Robert Vince, John Kilama, Phuong T. Pham, Scott A. Beers, Bonnie J. Bowdon, Kathy A. Keith, William B. Parker

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


A series of 6-alkoxy and 6-alkylamino carbovir derivatives were synthesized in order to evaluate prodrug approaches to increased bioavailability of the anti-HIV agent, carbovir. All of the compounds were active against HIV with the N-alkyl derivatives less active than the corresponding O-alkyl derivatives. The adenosine deaminase inhibitor, EHNA, had no effect on the anti-HIV activity of 6-propoxycarbovir, while the adenylic acid deaminase inhibitor, 2’ -deoxycoformycin, significantly decreased antiviral activity. These observations suggest that the 6-alkoxycarbovirs are metabolized directly to the monophosphates and are subsequently converted to carbovir monophosphate via adenylic acid deaminase.

Original languageEnglish (US)
Pages (from-to)1703-1708
Number of pages6
JournalNucleosides and Nucleotides
Issue number8
StatePublished - 1995

Bibliographical note

Funding Information:
Acknowledgments. This work was supported by Public Health Service Grant CA23263 from the National Cancer Institute and Grant A129157 from the National Institute of Allergy and Infectious Diseases.


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