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新型6-(3,5-二甲基苄基)尿嘧啶类似物作为潜在抗HIV-1药物的合成与评价

Synthesis and evaluation of novel 6-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents.

作者信息

Khalifa Nagy M, Pedersen Erik B, Nielsen Claus, Al-Omar Mohamed A

出版信息

Bioorg Khim. 2014 Sep-Oct;40(5):629-35. doi: 10.7868/s0132342314040058.

Abstract

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.

摘要

合成了一系列新型的在C-6位带有3,5-二甲基苄基的尿嘧啶衍生物,并将其作为非核苷类HIV-1逆转录酶抑制剂进行评价。化合物的纯度已通过薄层色谱法确证。这些化合物的结构是根据元素分析和光谱研究确定的。一些受试化合物对野生型HIV-1显示出中度至强效活性,且N-1烷基化衍生物具有高活性。

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