Synthesis and antiviral activity of amino acid carbamate derivatives of AZT.
Synthesis and antiviral activity of amino acid carbamate derivatives of AZT.
复制标题
AZT氨基酸氨基甲酸酯衍生物的合成及其抗病毒活性。
DOI：
10.1080/15257770008032998
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发表时间：
2000
期刊：
影响因子：
--
通讯作者：
Wagner,CR
中科院分区：
文献类型：
--
作者：
Chang,SL;Griesgraber,G;Abraham,TW;Garg,T;Song,H;Zimmerman,CL;Wagner,CR
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.
