三氮唑核苷及衍生物的设计合成与生物活性研究

Studies on Synthesis and Antiviral Activity of Ribavirin and Its Derivatives

以四乙酰核糖、1,2 ,4 三氮唑 3 羧酸甲酯为原料 ,经过缩合、氨解、保护、亲核取代、水解等五步反应得到 4个新的三氮唑核苷衍生物 4a～ 4d ,所有目标化合物的化学结构均经核磁共振氢谱、质谱或 (和 )元素分析所确正 .通过体外抗病毒活性测试表明 。

Four new ribavirin derivatives were synthesized. Tetra-acetylribofuranose reacts with 1,2,4-triazole-3-carboxylate through condensation, ammonolysis, protection, nucleophilic substitution and hydrolysis to give target compounds 4a similar to 4d. Some experimental parameters were discussed. Chemical structures of these four new compounds have been confirmed by means of H-1 NMR, MS spectra and elemental analysis. The results of bioactivity in vivo of these target compounds showed that two of the four new 5'-substituted ribavirin analogs have anti-influenza A activities to some extent.