6-O-烷基阿昔洛韦衍生物的合成及其抗病毒活性

Synthesis and antiviral activities of 6-O-alkyl acyclovir's derivatives

目的 以改善阿昔洛韦的水溶性为目的 ,设计并合成 6 -O -烷基阿昔洛韦衍生物 ,并测定其抗病毒活性。方法 以阿昔洛韦为先导化合物 ,合成一系列 6 -O -烷基阿昔洛韦衍生物 ,并以阿昔洛韦为阳性对照 ,进行体外抗HSV -I和HSV -II病毒的活性测定。结果 合成了 6 -O -烷基阿昔洛韦衍生物 10个 ,结构均经过元素分析、1HNMR和MS的确认。结论 部分目标化合物具有一定的体外抗HSV -I和HSV -II病毒的活性 。

OBJECTIVE To design and synthesize 6-O-alkyl acyclovir's(ACV's) derivatives, and test their antiviral activities. METHODS Using ACV as the leading compound ,a series of 6-O-alkyl ACV's derivatives were synthesized,and then their activities against HSV-I and HSV-II viruses were tested in vitro with ACV as the positive control. RESULTS 10 new compounds were synthesized,and their structures were all confirmed by the elementary analysis, 1HNMR and MS. CONCLUSION Some of the title compounds have a certain of activities against HSV-I and HSV-II in vitro, but their activities are weaker than that of ACV.