Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However,...Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.展开更多
目的观察中国HIV-1感染者在高效抗反转录病毒治疗（Highly active antiretroviral therapy，HAART）中，外周血HIV-1RNA、CD4＋T淋巴细胞数量和IL-2、IL-7的相关关系，探讨这些^y链细胞因子与抗HIV病毒免疫应答及其在病毒控制中的作用...目的观察中国HIV-1感染者在高效抗反转录病毒治疗（Highly active antiretroviral therapy，HAART）中，外周血HIV-1RNA、CD4＋T淋巴细胞数量和IL-2、IL-7的相关关系，探讨这些^y链细胞因子与抗HIV病毒免疫应答及其在病毒控制中的作用。方法2009年6月至2010年12月，35椤iI接受初次HAART的慢性HIV-1感染者被纳入本研究并随访48周，检测HAART治疗0、24、48周时的外周血HIV．1RNA定量、CD4＋T淋巴细胞数、IL-2以及IL-7水平，并分析其相关性。结果35例HIV．AIDS在HAART治疗前的IL-2水平[（9．67±2．6）pg／ml]明显低于正常对照值[（27．36±5．05）pg／ml]，在经过48周治疗后显著升高[（19．8±3．3）pg／ml]，而在HAART治疗前的IL-7水平[（81．74±20．47）pg／ml]明显高于正常对照值[（2．06±1．52）pg／ml]，在48周治疗后则显著降低[（8．36±2．16）pg／ml]。IL-2水平在HAART的0、48周与CD4＋细胞计数呈相同变化趋势但相关性不明显（O周：R=0．21，P=0．063；48周：R=0．19，P=0．103），24周呈正相关（R=0．24，P=0．033），而IL-7水平在HAART的0周与CD4＋细胞计数呈负相关（R=-0．28，P=0．012），在24、48周无相关。IL-2水平和HIVRNA病毒载量呈负相关（R=-0．17，P=0．032），而IL-7水平和HIV RNA病毒载量关系不明显（P=0．76）。结论48周HAART治疗中IL-2和IL-7水平均有明显变化。与CD4＋T细胞计数变化密切相关，与外周血HIV RNA水平有一定关系。提示这些细胞因子在免疫重建和病毒控制中起重要作用。展开更多
文摘Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.
