We report the synthesis of phosphoramidate conjugates of 3′-azido-3′-deoxythymidine (AZT) glycerolipid derivatives and amino acid esters. For the synthesized compounds, 50% inhibition of the HIV-1 MvP-899 strain in human T lymphoid MT-4 cells is achieved at concentrations of 0.014–0.356 µM. Significantly, compound 3c (which contained ethyl ester of α-alanine) was found to be the most active with EC₅₀ value 0.014 µM. We show that, among these glycerolipid derivatives of AZT, some compounds are less toxic than AZT, and also they possess a similar or higher selectivity index compared to AZT (SI = 11,643).

中文翻译：

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3'-叠氮基-3'-脱氧胸苷甘油脂衍生物和氨基酸酯的磷酸氨基甲酸酯偶联物：合成和抗HIV活性

我们报告了3'-叠氮基-3'-脱氧胸苷（AZT）甘油脂衍生物和氨基酸酯的氨基磷酸酯共轭物的合成。对于合成的化合物，在0.014–0.356 µM的浓度下，对人T淋巴细胞MT-4细胞中HIV-1 MvP-899菌株的抑制率为50％。显着地，发现化合物3c（包含α-丙氨酸的乙酯）最具活性，EC ₅₀值为0.014 µM。我们显示，在AZT的这些甘油脂衍生物中，某些化合物的毒性低于AZT，并且与AZT相比，它们具有相似或更高的选择性指数（SI = 11,643）。