Uckun Fatih M, Samuel P, Qazi S, Chen C, Pendergrass S, Venkatachalam T K
Department of Virology, Parker Hughes Institute, St. Paul, Minn., USA.
Antivir Chem Chemother. 2002 May;13(3):197-203. doi: 10.1177/095632020201300306.
We compared the anti-HIV activity of 13 phenyl phosphate derivatives of stavudine (2',3'-didehydro-2',3'-dideoxythymidine/d4T) by examining their ability to inhibit HIV-1 replication in human peripheral blood mononuclear cells. Our results show that the introduction of electron-withdrawing substituents enhances the activity of these phosphoramidate derivatives. The rate of chemical hydrolysis under alkaline conditions (but not the lipophilicity) predicted the potency of the compounds.
我们通过检测13种司他夫定（2'，3'-二脱氢-2'，3'-二脱氧胸苷/d4T）的苯基磷酸酯衍生物抑制HIV-1在人外周血单核细胞中复制的能力，比较了它们的抗HIV活性。我们的结果表明，吸电子取代基的引入增强了这些氨基磷酸酯衍生物的活性。碱性条件下的化学水解速率（而非亲脂性）预测了这些化合物的效力。
