新型6-(3,5-二甲基苄基)尿嘧啶类似物的合成与评价

Nagy M Khalifa, Erik B Pedersen, Claus Nielsen, Mohamed A Al-Omar
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引用次数: 0

摘要

在C-6位置上具有3,5-二甲基苄基的一系列新的尿嘧啶衍生物被合成并评估为非核苷类HIV-1逆转录酶抑制剂。用薄层色谱法证实了化合物的纯度。在元素分析和光谱研究的基础上确定了这些化合物的结构。部分化合物对野生型HIV-1具有中强活性,N-1烷基化衍生物具有高活性。
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Synthesis and evaluation of novel 6-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents.

A novel series of uracil derivatives with a 3,5-dimethylbenzyl group at the C-6 position were synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. Some of the tested compounds showed moderate to potent activities against wild-type HIV-1, and N-1 alkylated derivatives were highly active.

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