摘要
目的:修饰阿德福韦(ADV)结构,设计合成新化合物,研究其对乙肝病毒HBsAg、HBeAg的抑制活性。方法:以(ADV)为原料,经磷酰氯化、三氟乙醇酯化和氯甲酸酯缩合等反应,设计合成了未见文献报道的8个嘌呤类目标化合物1a-1h,所有化合物经1HNMR谱等确证;体外药理实验采用酶联免疫法(ELISA),阳性药物采用临床常用同类药物ADV。结果:设计合成的8个化合物,对HBsAg和HBeAg都有一定的抑制作用,其中化合物1d,1e,1g,1h对HBsAg抑制活性与ADV相当,化合物1g对HBeAg抑制活性与ADV相当。所有目标化合物对HBsAg抑制活性好于对HBeAg抑制活性。结论:在嘌呤环N6位引入较长碳链的1g活性最佳。
Objective：To study of design and synthesis of the new （ADV） derivatives and study their activities of inhibiting hepatitis B virus HBsAg and HBeAg. Methods：Starting with ADV, we synthesized 8 firstly reported purine compounds 1a-1h, which have been verified by NMR and MS. Enzyme-linked immunosorhent assay （ELISA） was used to assess HBsAg and HBeAg. The positive control is ADV. Results：The test results show the inhibitory rate of targeted purine compounds on HBsAg nad HBeAg is correspond with ADV. Conclusion： 1g introduced long carbon chain at N6 substituted of purine shows the best activity.
出处
《药学实践杂志》
CAS
2009年第6期426-429,共4页
Journal of Pharmaceutical Practice
基金
上海市2004年度重大科技攻关项目(2004DZ19209)
