阿昔洛韦的磷酰胺酯衍生物：在 HIV-1 和 HSV-1 模型中的体外抗病毒活性和合成。
Phosphoramidate derivatives of acyclovir: synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro.
机构信息
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 32 Vavilov St., Moscow, 119991, Russian Federation.
出版信息
Bioorg Med Chem. 2012 Oct 1;20(19):5802-9. doi: 10.1016/j.bmc.2012.08.008. Epub 2012 Aug 17.
The antiviral activity against HIV and HSV and the chemical stability of ACV phosphoramidate derivatives were studied. The phosphoramidates of ACV demonstrated moderate activity. The best compound appeared to be 9-(2-hydroxymethyl)guanine phosphoromonomorpholidate (7), which inhibited virus replication in pseudo-HIV-1 particles by 50% at 50 μM. It also inhibited replication of wild-type HSV-1 (9.7 μM) as well as an acyclovir-resistant strain (25 μM). None of the synthesised compounds showed any cytotoxicity.
研究了 ACV 膦酰胺酯衍生物对 HIV 和 HSV 的抗病毒活性和化学稳定性。ACV 的膦酰胺酯表现出中等活性。最好的化合物似乎是 9-(2-羟甲基)鸟嘌呤磷酰单吗啉酯（7），其在 50μM 时可抑制假 HIV-1 颗粒中病毒复制 50%。它还抑制野生型 HSV-1（9.7μM）和耐阿昔洛韦的菌株（25μM）的复制。所合成的化合物均无细胞毒性。
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