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6-O-取代苯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-substituted phenyl derivatives of aciclovir
【摘要】 目的设计合成 6 O 取代苯基阿昔洛韦衍生物 ,并进行抗病毒活性测定。方法以阿昔洛韦 (ACV)为先导化合物 ,对阿昔洛韦分子中的碱基进行结构修饰 ,合成一系列 6 O 取代苯基阿昔洛韦衍生物 ,并以阿昔洛韦为阳性对照进行体外抗HSV Ⅰ和HSV Ⅱ病毒活性测定。结果合成了 11个未见文献报道的 6 O 取代苯基阿昔洛韦衍生物 ,其结构均经元素分析、1H NMR和MS确证。结论部分目标化合物具有一定的体外抗HSV Ⅰ和HSV Ⅱ病毒活性 ,但较阿昔洛韦作用弱。
【Abstract】 Aim To design and synthesize 6-O-substituted phenyl derivatives of aciclovir(ACV),and to test their antiviral activities.Methods Using ACV as the lead compound,a series of 6-O-substituted phenyl derivatives of ACV were synthesized.Their activities against HSV-Ⅰ and HSV-Ⅱ viruses were tested in vitro with ACV as the positive control.Results Eleven new compounds were synthesized,and their structures were all confirmed by the elemental analysis,1H-NMR and MS detection.Conclusion Some of the title compounds have a certain extent of activities against HSV-Ⅰ and HSV-Ⅱ in vitro,but all of their activities are weaker than ACV′s.
【Key words】 medicinal chemistry; preparation; derivatization; aciclovir; antiviral activity;
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2005年01期
- 【分类号】R914;R965
- 【被引频次】3
- 【下载频次】199