核苷酸前药设计中核苷氢膦酰胺酯的研究。
Investigations of nucleoside H-phosphonamidate in the design of nucleotide prodrug.
作者信息
Egron D, Imbach J L, Gosselin G, Aubertin A M, Périgaud C
机构信息
Université Montpellier II, UMR 5625 CNRS, Montpellier, France.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):895-7. doi: 10.1081/NCN-120022680.
PMID:14565305
Abstract
The synthesis, anti-HIV activity and stability studies of a H-phosphonamidate derivative of 3'-azido-2',3'-dideoxythymidine (AZT) incorporating a N,N-diisopropylamino residue as first model of alkylamino group are reported. The results demonstrate that such phosphorylated structure exerts its biological effects via chemical hydrolysis into the corresponding H-phosphonate, precursor of the parent nucleoside.
摘要
报道了3'-叠氮基-2',3'-二脱氧胸苷（AZT）的一种含N,N-二异丙基氨基残基作为烷基氨基基团首个模型的H-膦酰胺酯衍生物的合成、抗HIV活性及稳定性研究。结果表明，这种磷酸化结构通过化学水解为相应的H-膦酸酯（母体核苷的前体）发挥其生物学效应。
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