TY - JOUR
T1 - Synthesis and antiviral activity of amino acid carbamate derivatives of AZT
AU - Chang, Shu Ling
AU - Griesgraber, George
AU - Abraham, Timothy W.
AU - Garg, Tullika
AU - Song, Heng
AU - Zimmerman, Cheryl L.
AU - Wagner, Carston R.
PY - 2000/1/1
Y1 - 2000/1/1
N2 - 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.
AB - 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.
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U2 - 10.1080/15257770008032998
DO - 10.1080/15257770008032998
M3 - Article
C2 - 10772704
AN - SCOPUS:0034014407
VL - 19
SP - 87
EP - 100
JO - Nucleosides, Nucleotides and Nucleic Acids
JF - Nucleosides, Nucleotides and Nucleic Acids
SN - 1525-7770
IS - 1-2
ER -