Abstract
Lipophilic amino acid methyl ester and methyl amide carbamates of 3'- azido-3'-deoxythymidine (AZT) were synthesized and their anti-HIV-1 activity in PBMCs was determined. The methyl amides were more potent (EC50s = 1.8 - 4.0 μM) than the methyl esters (EC50s = 2.0 - 20 μM). Carbamate hydrolysis by cell lysates and liberation of AZT was not observed for representative methyl ester or methyl amide AZT carbamates. No evidence of direct inhibition of HIV reverse transcriptase or integrase was observed.
Original language | English (US) |
---|---|
Pages (from-to) | 87-100 |
Number of pages | 14 |
Journal | Nucleosides, Nucleotides and Nucleic Acids |
Volume | 19 |
Issue number | 1-2 |
DOIs | |
State | Published - 2000 |
Bibliographical note
Funding Information:Partial financial support is gratefully acknowledged from NIH (CA61908), Advanced Magnetics, Inc., and the University of Mmnesota Graduate School. We also wish to thank Dr. Christophe Marchand and Dr. Yves Pommier of the National Institutes of Health for carrying out the integrase inhibition assays.