Danel K, Nielsen C, Pedersen E B
Department of Chemistry, Odense University, Denmark.
Acta Chem Scand (Cph). 1997 Mar;51(3 Suppl):426-30. doi: 10.3891/acta.chem.scand.51-0426.
5-Ethyl-6-(1-naphthylmethyl)uracil and 5-ethyl-6-(1-naphthylmethyl)-2-thiouracil were alkylated to give, respectively. N-1 and S2, ethoxymethyl and methylthiomethyl uracil derivatives. 5-Ethyl-6-(1-naphthylmethyl)-2-thiouracil was also S2 alkylated with methyl bromoacetate. The products showed activity against HIV-1, and the N-1 alkylated derivatives were indeed highly active.
5-乙基-6-(1-萘甲基)尿嘧啶和5-乙基-6-(1-萘甲基)-2-硫尿嘧啶分别被烷基化,得到N-1和S2的乙氧基甲基及甲硫基甲基尿嘧啶衍生物。5-乙基-6-(1-萘甲基)-2-硫尿嘧啶也用溴乙酸甲酯进行了S2烷基化。这些产物显示出对HIV-1的活性,并且N-1烷基化衍生物确实具有高活性。