Synthesis and anti-retroviral activity of O,O'-bis(3'-azido-2',3'-dideoxythymidin-5'-yl) phosphoramidate derivatives.

I Kers, J Stawiński, J L Girardet, J L Imbach, C Périgaud, G Gosselin, A M Aubertin
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引用次数: 8

Abstract

A simple and efficient protocol for the preparation of various symmetrical dinucleoside phosphoramidates derived from AZT, is presented. It consists of the phosphonylation of AZT with phosphonic acid in the presence of DCC to produce the symmetrical H-phosphonate diester, followed by its oxidative conversion to various phosphoramidate analogues. The synthesized compounds were evaluated for their anti-HIV activity in different cell cultures.

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O,O'-双(3'-叠氮-2',3'-二脱氧胸腺苷-5'-酰基)磷酰胺衍生物的合成及其抗逆转录病毒活性
本文提出了一种简单有效的方法,用于制备由AZT衍生的各种对称二核苷磷酸酯。它包括AZT与磷酸在DCC存在下的膦化反应,生成对称的h -膦酸二酯,然后氧化转化为各种磷酸酰胺类似物。合成的化合物在不同的细胞培养中对其抗hiv活性进行了评价。
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